Catalog No.
Product Name
Application
Product Information
Citations
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FGFR4 Inhibitor
FGFR4-IN-13 is a selective inhibitor of fibroblast growth factor receptor 4 (FGFR4), primarily involved in the regulation of cellular proliferation and survival pathways. This compound demonstrates notable anti-tumor activity, making it a valuable tool for investigating hepatocellular carcinoma. FGFR4-IN-13 facilitates research aimed at understanding the molecular underpinnings of this cancer type and developing targeted therapeutic strategies. -
FGFR Modulator
SUN13837 is a potent orally active modulator of fibroblast growth factor receptors (FGFRs) with the ability to penetrate the blood-brain barrier. It exhibits neuroprotective properties, making it relevant for research in neurodegenerative diseases. This compound can serve as a valuable tool for investigating therapeutic interventions in FGFR-related neurological conditions. -
FGFR-4 Inhibitor
FGFR4-IN-16 is a selective covalent inhibitor targeting the fibroblast growth factor receptor 4 (FGFR-4). It demonstrates potent activity in disrupting FGFR-4 signaling pathways, making it relevant for cancer research. This compound may be utilized in studies investigating the role of FGFR-4 in tumor growth and progression, providing valuable insights into therapeutic strategies for FGFR-4-dependent malignancies. -
FGFR Inhibitor
FGFR-IN-5 is a selective inhibitor of fibroblast growth factor receptor (FGFR), a critical tyrosine kinase receptor implicated in various cancer pathways. This compound demonstrates significant biological activity in inhibiting FGFR signaling, making it valuable for cancer research applications. Additionally, FGFR-IN-5 possesses an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), thus serving as a versatile click chemistry reagent for further molecular investigations. -
FGFR Inhibitor
FGFR-IN-11 is a potent covalent inhibitor of Fibroblast Growth Factor Receptors (FGFR), demonstrating IC50 values of 9.9 nM for FGFR1, 3.1 nM for FGFR2, 16 nM for FGFR3, and 1.8 nM for FGFR4. This compound effectively hinders the proliferation of various cancer cell lines at nanomolar concentrations and significantly reduces tumor growth in xenograft mouse models. FGFR-IN-11 serves as a valuable tool for research into targeted cancer therapies and the underlying mechanisms of FGFR-mediated tumorigenesis. -
FGFR4 Inhibitor
FGFR4-IN-12 is a selective inhibitor targeting Fibroblast Growth Factor Receptor 4 (FGFR4), demonstrating enhanced potency and specificity. This compound exhibits significant anti-proliferative effects against FGFR4-dependent hepatocellular carcinoma (HCC) cell lines, making it valuable for cancer research. Additionally, FGFR4-IN-12 features an alkyne functional group, enabling its use as a click chemistry reagent that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
FGFR Inhibitor
FGFR-IN-13 is an irreversible covalent inhibitor of fibroblast growth factor receptors (FGFR), specifically targeting FGFR1 (IC50 = 0.20 ± 0.02 nM) and FGFR4 (IC50 = 0.40 ± 0.03 nM). This compound modulates FGFR-mediated signaling pathways by downregulating total PARP and Bcl-2 protein levels while promoting the expression of Cleaved-PARP and Bax in a dose-dependent manner. FGFR-IN-13 exhibits significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications involving FGFR signaling pathways. -
FGFR Inhibitor
FGFR-IN-22 is a potent FGFR inhibitor, demonstrating IC50 values of 0.631 nM for FGFR1, 1.26 nM for FGFR2, 0.851 nM for FGFR3, and 1 nM for FGFR4. This compound effectively inhibits cell proliferation linked to FGFR1 and FGFR3 signaling pathways, making it a valuable tool for research in cancer types such as chronic lymphocytic leukemia (CLL). FGFR-IN-22 is useful for studying the role of FGFRs in tumor biology and therapeutic development. -
FGFR4 Inhibitor
FGFR4-IN-6 is a covalent, reversible inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4), exhibiting an IC50 value of 5.4 nM. It demonstrates significant antitumor activity by inducing tumor regressions in a xenograft mouse model using the Hep3B2.1-7 hepatocellular carcinoma cell line, while maintaining a favorable toxicity profile. Additionally, FGFR4-IN-6 serves as a click chemistry reagent, featuring an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds, making it a valuable tool for chemical biology applications. -
EGFR Inhibitor
EGFR-IN-47 is a potent orally active inhibitor of the EGFR L858R/T790M/C797S mutations, with an IC50 of 0.01 μM. This compound effectively induces cell cycle arrest and promotes apoptosis in cancer cells. EGFR-IN-47 holds significant potential for research applications related to non-small cell lung cancer (NSCLC). -
EGFR Inhibitor
EGFR-IN-78 is a reversible inhibitor of the EGFR variant C797S-TK, classified as a 2-aminopyrimidine derivative. This compound induces apoptosis and exhibits significant anti-proliferative activity by inhibiting EGFR phosphorylation. Additionally, EGFR-IN-78 effectively arrests the cell cycle at the G2/M phase, making it a valuable tool for research applications focused on targeted cancer therapies. -
EGFR-TK Inhibitor
EGFR-TK-IN-4 is a potent and selective inhibitor of the epidermal growth factor receptor tyrosine kinase (EGFR-TK). It has been demonstrated to induce apoptosis in cancer cells and exhibits significant antitumor activity. This compound is suitable for studying EGFR signaling pathways and developing targeted therapies in oncology research. -
EGFR Inhibitor
YS-363 is a potent and selective orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.96 nM for wild-type and 0.67 nM for the L858R mutant form. This compound effectively induces G0/G1 cell cycle arrest and promotes apoptosis in target cells. YS-363 is valuable for research applications focused on cancer therapeutics and the molecular mechanisms of EGFR signaling. -
PDGFR Inhibitor
PDGFR-IN-1 is a potent inhibitor of the platelet-derived growth factor receptor (PDGFR), exhibiting IC50 values of 2.4 nM for PDGFRα and 0.9 nM for PDGFRβ. This compound demonstrates significant antitumor activity while maintaining low toxicity, making it a valuable tool for research applications in osteosarcoma studies. Its selectivity for PDGFR allows for detailed investigations into tumor growth mechanisms and therapeutic interventions. -
FGFR2 Degrader
PROTAC FGFR2 degrader 1 is a specialized degrader designed to selectively target and degrade FGFR2, exhibiting a DC50 of 6.46 nM and an FGFR2 IC50 of 0.08 nM. This compound demonstrates significant anti-proliferative activity, inducing G0/G1 cell cycle arrest in KATOIII and SNU16 cell lines while inhibiting apoptosis through modulation of downstream signaling proteins, p-ERK and p-PLCγ. In in vivo studies, PROTAC FGFR2 degrader 1 effectively suppresses the growth of SNU16 xenograft tumors, showcasing its potential for research in gastric cancer therapeutic applications. -
EGFRC797S-TK Inhibitor
Os30 is a potent fourth-generation EGFR inhibitor specifically targeting the EGFRC797S-TK mutation. With IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively, Os30 effectively inhibits EGFR phosphorylation, induces G1 phase cell cycle arrest, and triggers apoptosis in KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. This compound demonstrates significant antitumor activity in non-small cell lung cancer (NSCLC) harboring the EGFRC797S mutation, making it a valuable tool for cancer research and therapeutic exploration. -
Pan-HER Inhibitor
pan-HER-IN-2 is a reversible, orally active pan-HER inhibitor targeting multiple receptor tyrosine kinases, with IC50 values of 0.72 nM for EGFR, 2.0 nM for HER4, 8.2 nM for EGFRT790M/L858R, and 75.1 nM for HER2. This compound effectively induces apoptosis and exhibits significant antitumor activities. pan-HER-IN-2 is suitable for research applications focused on cancer therapy and the exploration of targeted treatments for HER family receptor-positive tumors. -
ALK/EGFR Degrader
SIAIS164018 is a PROTAC-based degrader targeting ALK and EGFR, demonstrating IC50 values of 2.5 nM and 6.6 nM against ALK and ALK G1202R, respectively. This compound exhibits potent inhibitory effects on cancer cell migration and invasion, induces G1 cell cycle arrest, and promotes apoptosis. SIAIS164018 is a valuable tool for research applications investigating targeted degradation mechanisms in oncology. -
Intermediate
KTX-582 intermediate-1 is a crucial intermediate in the synthesis of KTX-582, serving as a key component for antibody-drug conjugate (ADC) preparation. KTX-582 functions as an IRAK4 degrader, effectively inducing apoptosis with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. This compound is instrumental for research applications focused on targeting IRAK4-related pathways and exploring therapeutic strategies in various cancers. -
EGFR Inhibitor
Gefitinib dihydrochloride is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 of 33 nM. This compound effectively inhibits EGF-stimulated tumor cell proliferation (IC50 of 54 nM) and prevents EGFR autophosphorylation, thereby blocking downstream signaling pathways. Gefitinib dihydrochloride is valuable for cancer research, particularly in the study of lung and breast cancers, due to its ability to induce autophagy and promote apoptosis in tumor cells. -
EGFR Inhibitor
Zorifertinib hydrochloride is a potent orally active inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 0.3 nM, 0.2 nM, and 0.2 nM against wild-type EGFR, EGFR L858R, and EGFR exon 19 deletion variants, respectively. This compound is capable of inducing apoptosis in cancer cells and exhibits significant antitumor activity. Zorifertinib hydrochloride is primarily utilized in research related to non-small cell lung cancer (NSCLC) and hepatocellular carcinoma (HCC). -
VEGFR2/MET Inhibitor
Cabozantinib hydrochloride is a potent inhibitor of VEGFR2 and MET, exhibiting IC50 values of 0.035 nM and 1.3 nM, respectively. Additionally, it effectively inhibits other receptor tyrosine kinases including KIT, RET, AXL, TIE2, and FLT3 with IC50 values of 4.6 nM, 5.2 nM, 7 nM, 14.3 nM, and 11.3 nM. This compound demonstrates significant antiangiogenic properties by disrupting tumor vasculature and inducing apoptosis in both tumor and endothelial cells. It is widely utilized in cancer research to explore the mechanisms of tumor progression and treatment resistance. -
JAK2/FLT3 Inhibitor
Flonoltinib sulfate is a potent, orally active dual inhibitor targeting JAK2 and FLT3. It demonstrates significant biological activity with IC50 values of 0.7 nM for JAK2 and 4 nM for FLT3, along with activity against JAK1 and JAK3 at 26 nM and 39 nM, respectively. This compound is primarily utilized in cancer research, particularly in the study of hematological malignancies influenced by aberrant JAK2 and FLT3 signaling pathways. -
IRAK4 Inhibitor
Emavusertib hydrochloride is an orally active inhibitor targeting IRAK4, with an IC50 of 57 nM, and FLT3. This compound effectively inhibits NF-κB and MyD88 signaling pathways, resulting in decreased production of pro-inflammatory cytokines such as IL-6 and IL-10. Its anti-inflammatory and anti-proliferative properties make it a valuable tool for cancer research, as it promotes apoptosis in cancer cells and demonstrates antitumor efficacy in mouse model studies. -
ALK/ROS1 Inhibitor
Lorlatinib acetate is a selective and orally active inhibitor targeting ROS1 and ALK pathways. This compound exhibits potent anticancer activity with Kis of less than 0.025 nM for ROS1 and less than 0.07 nM for wild-type ALK, establishing it as a promising therapeutic candidate for ALK-driven cancers. Additionally, Lorlatinib acetate effectively inhibits ALK phosphorylation, demonstrated by IC50 values ranging from 15-43 nM for ALKL1196 and varying efficacy against multiple resistant mutations, making it a valuable tool for cancer research and drug discovery. -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib malate is an orally active, multi-targeted kinase inhibitor primarily targeting c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This compound induces cell apoptosis and demonstrates significant anti-tumor activity in human gastric cancer cells and xenograft models. Famitinib malate is a valuable tool for research into cancer therapies and mechanisms of action. -
VEGFR2/KDR Inhibitor
Vatalanib hydrochloride is a potent and selective inhibitor of VEGFR2 (vascular endothelial growth factor receptor 2), with an IC50 of 37 nM. It effectively penetrates the blood-brain barrier, making it suitable for studies involving central nervous system applications. Vatalanib hydrochloride is utilized in research focused on angiogenesis, tumor growth inhibition, and vascular biology, contributing valuable insights into therapeutic strategies for various cancers. -
FLT3 Inhibitor
Tuspetinib hydrate is a selective FLT3 inhibitor that demonstrates IC50 values of 1.1 nM, 1.8 nM, and 1.0 nM against FLT3 wild-type, FLT3 internal tandem duplication (ITD), and FLT3 D835Y kinases, respectively. As a reversible type I inhibitor, Tuspetinib hydrate effectively modulates key signaling pathways, including p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. This compound exhibits potent anti-leukemic activity by inhibiting cell proliferation and inducing apoptosis in leukemic cells, making it a valuable tool for research in leukemia and related hematological malignancies. -
FAK/FGFR2 Inhibitor
PHM16 is an ATP-competitive inhibitor targeting Focal Adhesion Kinase (FAK) and Fibroblast Growth Factor Receptor 2 (FGFR2), with IC50 values of 0.4 μM and 0.37 μM, respectively. This compound exhibits strong anti-angiogenic properties, making it a valuable tool for studies focused on inhibiting tumor angiogenesis and understanding related signaling pathways. Its dual inhibition profile positions PHM16 as an important reagent for cancer research and therapeutic development targeting angiogenesis-related mechanisms. -
EGFR Inhibitor
SKLB188 is a potent and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 5 nM. This compound effectively suppresses both MEK/Erk and Akt/mTOR signaling pathways, leading to reduced proliferation of head and neck squamous cell carcinoma (HNSCC) and inducing caspase-dependent apoptosis. SKLB188 is a valuable reagent for research focused on EGFR-overexpressing solid tumors. -
EGFR Inhibitor
EGFR-IN-59 is an epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 190 nM, demonstrating apoptosis-inducing properties. This compound exhibits significant cytotoxicity against non-small cell lung cancer cell lines (A549) with an IC50 of 8.62 µM, while maintaining a lower cytotoxic effect on normal lung fibroblasts (WI38) at 52.6 µM. EGFR-IN-59 is a valuable tool for investigating various cancers, including non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer, and colorectal cancer. -
ALK/EGFR Inhibitor
ALK/EGFR-IN-1 is a potent dual inhibitor targeting ALK and EGFR, effectively blocking their phosphorylation. This compound demonstrates high inhibitory activity against EGFR L858R T790M mutants in H1975 cells, with an IC50 of 4.3 nM, and EML4-ALK in BaF3 cells, with an IC50 of 3.6 nM. ALK/EGFR-IN-1 is particularly valuable for research in non-small cell lung cancer (NSCLC) and provides insights into the mechanisms of resistance in targeted therapies. -
Pan-HER Inhibitor
pan-HER-IN-1 is an irreversible pan-HER inhibitor that targets multiple human epidermal growth factor receptors (HER) with IC50 values of 0.38 nM for EGFR, 1.6 nM for HER4, 2.2 nM for EGFRT790M/L858R, and 3.5 nM for HER2. This compound effectively induces apoptosis and exhibits significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications aimed at HER-driven malignancies. -
Multiple Kinase Inhibitor
KRC-108 is a potent aminopyridine that functions as a multiple kinase inhibitor, targeting c-Met and its variants, Ron, Flt3, and TrkA with IC50 values ranging from 3 nM to 80 nM. It demonstrates significant biological activity by inducing cell cycle arrest, promoting apoptotic cell death, and facilitating autophagy. KRC-108 showcases robust anti-tumor effects in vivo, particularly in HT29 colorectal cancer and NCI-H441 lung cancer xenograft models using athymic BALB/c nu/nu mice, making it a valuable reagent for cancer research applications. -
VEGFR-2 Inhibitor
VEGFR-2-IN-15 is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), a key regulator of angiogenesis. This compound effectively arrests cell growth in HepG2 cells at the Pre-G1 phase and induces apoptosis. It is a valuable tool for research applications focused on cancer biology and therapeutic strategies targeting angiogenesis. -
GLUT1/EGFR Inhibitor
GLUT1/EGFR-IN-1 is a potent inhibitor of both the GLUT1 transporter and the EGFR tyrosine kinase. By targeting the ATP-binding site of EGFR and concurrently inhibiting GLUT1-mediated energy metabolism, GLUT1/EGFR-IN-1 effectively reduces ATP levels, mitochondrial membrane potential, and intracellular lactic acid, while also preventing EGFR nuclear translocation. This compound is applicable in research focusing on nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC). -
FLT3-PROTAC Degrader
PROTAC FLT-3 degrader 4 is a CRBN-based degrader that selectively targets FLT3-ITD mutants by harnessing the ubiquitin-proteasome system for degradation. This compound demonstrates potent activity against FLT3-ITD mutant acute myeloid leukemia (AML) cells, offering a focused approach for research applications in cancer therapeutics. Its oral bioavailability positions it as a valuable tool for investigating FLT3-related signaling pathways and potential treatment strategies in AML. -
FLT3 Inhibitor
HI042 is a selective inhibitor of FMS-like Tyrosine Kinase 3 (FLT3), demonstrating potent activity with IC50 values of 0.62 μM in MOLM-13, 0.33 μM in MV4-11, and 0.89 μM in OCI-AML3 cell lines. This compound effectively reduces the viability of FLT3-internal tandem duplication (FLT3-ITD) mutation-positive cells, induces apoptosis, disrupts cell cycle progression, and diminishes clonogenic potential. HI042 serves as a valuable reagent in the research of acute myeloid leukemia (AML). -
IGF2BP2 Inhibitor
CWI1-2 is an inhibitor of IGF2BP2 that disrupts its interaction with m6A-modified target transcripts. This compound induces apoptosis and differentiation in responsive cells, showcasing potential anti-leukemic activity. CWI1-2 is valuable for research focused on the regulation of RNA metabolism and cancer biology, particularly in leukemia studies. -
TLR9 Agonist
Agatolimod is a Toll-like receptor 9 (TLR9) agonist and immunomodulator with an EC50 of 180 nM. It activates TLR9 and upregulates TLR6 expression, initiating downstream signaling through IRAK4, IRF5, and IRF7. Agatolimod enhances Th1-type immune responses and promotes the activation of various immune cells, leading to increased antigen presentation, antibody regulation, cytokine secretion, apoptosis, and enhanced cytotoxicity. This compound is relevant for research into COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis. -
SERT/NET Inhibitor
Amitriptyline is a tricyclic antidepressant that primarily inhibits the serotonin transporter (SERT) and norepinephrine transporter (NET), enhancing synaptic levels of serotonin and norepinephrine. With a Ki value of 3.45 nM for SERT and 13.3 nM for NET, Amitriptyline demonstrates significant antidepressant activity. Additionally, it exhibits agonistic properties at α2A adrenergic and TrkA/TrkB receptors, contributing to its analgesic and neurotrophic effects. Furthermore, Amitriptyline interacts with various receptors, including muscarinic cholinergic and H1 receptors, which may lead to a variety of side effects, while its ability to block sodium channels and hERG potassium channels raises concerns regarding cardiotoxicity. -
ALKBH5 Inhibitor
DDO-2728 is a selective inhibitor of AlkB homologue 5 (ALKBH5), demonstrating an IC50 of 2.97 μM. This compound enhances the levels of N6 methyladenosine (m6A) modifications, leading to increased cell apoptosis and cell cycle arrest. DDO-2728 has shown efficacy in suppressing tumor growth in the MV4 11 xenograft model, highlighting its potential application in cancer research and therapeutic strategies targeting ALKBH5. -
IGF2BP1 Inhibitor
AVJ16 is an inhibitor of the insulin-like growth factor 2 mRNA binding protein IGF2BP1, exhibiting a Kd of 1.4 μM. This compound disrupts the interaction between IGF2BP1 and its target mRNA, thereby modulating gene expression and translation processes. AVJ16 is valuable for research applications focused on cancer cell migration and the underlying mechanisms of IGF2BP1 in various malignancies. -
ALK Inhibitor
Neladalkib is a potent oral selective inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of 2.8 nM. This compound induces apoptotic cell death and demonstrates anti-tumor activity, making it a valuable tool for cancer research. Neladalkib is particularly relevant in studies focused on ALK-driven malignancies and therapeutic resistance mechanisms. -
Ligand for E3 Ligase
Thalidomide 5-fluoride is a thalidomide-derived ligand for the E3 ubiquitin ligase Cereblon, enabling targeted protein degradation via the PROTAC approach. This compound can be conjugated with specific target protein ligands, such as IRAK4, to create PROTAC molecules for enhanced therapeutic applications. Notably, PROTAC IRAK4 degrader-1 demonstrated significant IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, achieving degradation levels of <20%, >20-50%, and >50%, respectively. This underlines its potential utility in cellular studies of protein regulation and targeted therapeutics. -
IGF2BP3 Inhibitor
I3IN-002 is a small-molecule inhibitor of the RNA-binding protein IGF2BP3, exhibiting an IC50 of approximately 2 μM in SEM cells. By disrupting the interaction with m6A-modified mRNAs, I3IN-002 destabilizes the expression of key oncogenes, such as CDK6, MYC, and BCL2, leading to inhibition of leukemic cell proliferation, induction of cell cycle arrest, and promotion of apoptosis. This compound is a valuable tool for research focused on B-cell acute lymphoblastic leukemia. -
IRAK Inhibitor
KME-2780 is an orally active inhibitor targeting IRAK1 and IRAK4, exhibiting IC50 values of 19 nM and 0.5 nM, respectively. It plays a crucial role in the modulation of innate immune signaling pathways, making it a valuable tool for investigating dysregulation associated with hematologic malignancies and related disorders. Researchers can utilize KME-2780 to explore the therapeutic potential of IRAK inhibition in various immunological contexts. -
IGF2BP2 Inhibitor
CWI1-2 hydrochloride is an inhibitor of IGF2BP2, a protein that plays a crucial role in regulating m6A-modified target transcripts. By binding to IGF2BP2, CWI1-2 hydrochloride disrupts its interaction with these transcripts, thereby inducing apoptosis and promoting differentiation in cells. This compound demonstrates significant potential for therapeutic applications in leukemia research. -
PROTAC FGFR2 Degrader
LC-MB12 is an orally active PROTAC compound that targets FGFR2 degradation, with a DC₅₀ of 11.8 nM. It consists of the FGFR2 inhibitor BGJ398, a PROTAC linker, and a cereblon (CRBN) ligand. LC-MB12 effectively inhibits FGFR2 signaling in gastric cancer cells and exhibits antitumor activity. - ATWLPPR peptide is a biologically active heptapeptide and a specific antagonist of VEGFR2 (KDR/Flk-1). It binds to VEGFR2, completely blocking VEGF binding and thereby inhibiting VEGF-induced angiogenesis in vivo. ATWLPPR selectively inhibits human endothelial cell proliferation in vitro and fully suppresses VEGF-mediated angiogenesis in vivo.
