Catalog No.
Product Name
Application
Product Information
Citations
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Raf/VEGFR3 inhibitor
Sorafenib D4 (Bay 43-9006 D4) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively. -
Raf kinase inhibitor
B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively. -
raf kinase inhibitor
Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research. -
PROTAC B-Raf Degrader
PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) that facilitates the degradation of B-Raf through a Cereblon ligand. This compound demonstrates significant anti-cancer activity, making it a valuable tool for cancer research. It is particularly useful in studies investigating B-Raf-mediated signaling pathways and therapeutic strategies targeting oncogenic mutations in B-Raf. -
BRAFV600E Degrader
Tagarafdeg is a CRBN-based bifunctional degradation activating compound (BiDAC) selectively targeting BRAFV600E mutations. Demonstrating potent activity with a DC50 of 14 nM in A375 cells, it effectively degrades various BRAF mutations, including G469A and G466V, as well as the p61-BRAFV600E splice variant. This reagent is suitable for applications in tumor research, contributing to the understanding of BRAF-mediated oncogenic processes. -
BRAF-V600E Degrader
PROTAC BRAF-V600E degrader-1 is an effective degrader of the BRAF-V600E mutant, selectively targeting this oncogenic variant while sparing wild-type BRAF. With Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively, this compound facilitates degradation of BRAF-V600E through the ubiquitin-proteasome system (UPS). Its potent activity against melanoma cells makes it a valuable tool for research into targeted cancer therapies and mechanisms of drug resistance in BRAF-mutant tumors. -
RAF PROTAC Degrader
SJF-0628 is a RAF PROTAC degrader that facilitates the targeted degradation of BRAF protein in cancer cell lines, specifically in colorectal cancer models (Colo-205, LS-411N, HT-29, RKO) and the triple-negative breast cancer line DU-4475. This compound significantly reduces levels of phosphorylated MEK and ERK in DU-4475 cells, demonstrating notable anti-tumor activity. SJF-0628 is valuable for research studies focused on the mechanisms of colorectal cancer and triple-negative breast cancer. -
Tyrosinase Inhibitor
Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells. -
RAF-1/HIF-1α Inhibitor
MO-2097 is a selective RAF-1 and HIF-1α inhibitor that induces the destabilization of RAF-1, resulting in decreased levels of epithelial-mesenchymal transition (EMT) transcription factors and mesenchymal markers. Additionally, MO-2097 effectively inhibits HIF-1α protein expression mediated by hnRNPA2B1 in hypoxic conditions. This compound promotes the generation of mitochondrial reactive oxygen species (ROS), contributing to apoptosis in malignant cells. MO-2097 demonstrates significant potential in suppressing colorectal cancer metastasis by targeting the RAF/MEK/ERK signaling pathway and has shown efficacy in reducing tumor growth in HCT116 cell xenograft mouse models, thus serving as a valuable tool for colorectal cancer research. -
PI3K/Akt/Ras/Raf/MAPK Inhibitor
Erufosine is a potent inhibitor of the PI3K/Akt and Ras/Raf/MAPK signaling pathways. It demonstrates significant cytotoxic activity against breast cancer cell lines, specifically MCF-7 and MDA-MB-231, with IC50 values of 40.95 μM and 40.8 μM, respectively. By reducing the phosphorylation levels of PI3K (p85), Akt (PKB), and cRaf, Erufosine serves as a valuable tool in the research of breast cancer and myeloid leukemia. -
RAF/DDR Inhibitor
PHI-501 is a dual inhibitor targeting RAF and DDR pathways. It demonstrates potent anti-proliferative effects in melanoma cell lines, effectively inhibiting colony formation in drug-resistant cells. PHI-501 disrupts ERK and AKT phosphorylation and downregulates key gene sets associated with TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways, as well as pathways involved in epithelial-mesenchymal transition. In vivo studies show significant anti-tumor efficacy in the SK-MEL3DR xenograft model, making PHI-501 valuable for research on drug resistance in melanoma. -
Raf/EGFR Inhibitor
Lifirafenib maleate is a potent inhibitor of Raf kinase and EGFR, exhibiting IC50 values of 23 nM and 29 nM for recombinant BRafV600E and EGFR, respectively. This compound effectively disrupts critical signaling pathways involved in cancer cell proliferation and survival. Lifirafenib maleate is relevant for research applications in cancer biology, particularly in studies focusing on targeted therapies for tumors with BRAF mutations or EGFR dysregulation. -
EGFR/BRAF Inhibitor
EGFR/BRAF-IN-1 is a selective inhibitor targeting both EGFR and BRAFV600E with an IC50 of 45 nM. This compound, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, effectively inhibits cancer cell proliferation with a GI50 of 35 nM. Additionally, EGFR/BRAF-IN-1 exhibits notable antioxidant properties, making it a valuable reagent for research in cancer biology and therapeutic development. -
RAF Inhibitor
CCT241161 is a potent pan-RAF inhibitor that effectively targets multiple RAF family members with IC50 values of 3 nM for LCK, 6 nM for CRAF, 10 nM for SRC, 15 nM for V600E-BRAF, and 30 nM for BRAF. This compound demonstrates significant antiproliferative activity in BRAF and NRAS mutant melanoma cell lines, making it a valuable tool for cancer research. CCT241161 is relevant for studies focused on targeted therapies in oncogenic signaling pathways. -
Rb-Raf-1 Inhibitor
RRD-251 is a selective inhibitor of the retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction. This compound exhibits potent anti-proliferative, anti-angiogenic, and anti-tumor activities, making it valuable for research focused on cancer biology and therapeutic strategies targeting cell growth and tumor progression. Its ability to disrupt this critical protein interaction highlights its potential use in studies investigating the molecular mechanisms underlying various cancers. -
FGFR3/BRAF Binder
2,4,3',4',6'-Penta-O-(3-methylbutanoyl)sucrose functions as a selective binder for Fibroblast Growth Factor Receptor 3 (FGFR3) and BRAF, playing a pivotal role in modulating pathways associated with cancer progression. Derived from Atractylodes japonica, this compound exhibits low cytotoxicity towards cancer cell lines, making it a suitable candidate for research applications focused on targeted cancer therapies and signaling pathway studies. Its unique structural characteristics enhance its potential for further exploration in drug development and therapeutic interventions. -
Raf Inhibitor
ML786 is a potent Raf inhibitor with oral bioavailability, demonstrating IC50 values of 2.1 nM for V600EΔB-Raf, 4.2 nM for wild-type B-Raf, and 2.5 nM for C-Raf. Additionally, ML786 exhibits inhibitory effects on Abl-1, DDR2, EPHA2, KDR, and RET, with IC50 values under 0.5 nM, 7.0 nM, 11 nM, 6.2 nM, and 0.8 nM, respectively. This compound is suitable for research applications focused on cancer biology, helping to advance understanding of therapeutic targets within malignancies. -
PDGFRβ/B-Raf Inhibitor
KG5 is an orally active dual inhibitor targeting PDGFRβ and B-Raf through allosteric mechanisms. It also exhibits inhibitory effects on Flt3, KIT, and c-Raf. KG5 demonstrates significant anticancer and antiangiogenic activities, making it a valuable reagent for research in cancer therapy and angiogenesis studies. -
B-Raf Inhibitor
INU-152 is a potent and selective inhibitor of B-Raf, a key kinase in the MAPK signaling pathway. This compound effectively reduces tumor cell proliferation, enhances autophagy, and induces apoptosis through the inhibition of B-Raf activity. INU-152 demonstrates significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3), making it a valuable tool for cancer research applications. -
B-Raf Inhibitor
B-Raf IN 9 is a potent B-Raf inhibitor with an IC50 of 24.79 nM, targeting the B-Raf signaling pathway. This compound induces apoptosis and causes cell cycle arrest at the G2/M phase. B-Raf IN 9 demonstrates significant antitumor activity against the human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM, making it a valuable tool for cancer research and therapeutic investigations. -
EGFR/BRAFV600E Inhibitor
EGFR/BRAFV600E-IN-1 is a potent dual inhibitor targeting EGFR and the BRAFV600E mutation, with IC50 values of 0.08 µM and 0.15 µM, respectively. This compound effectively induces apoptosis and induces cell cycle arrest in the pre-G1 and G2/M phases. Additionally, it demonstrates significant antiproliferative activity against A-549, MCF-7, Panc-1, and HT-29 cell lines, with IC50 values of 1.2 µM, 0.79 µM, 1.3 µM, and 1.23 µM, respectively, making it valuable for cancer research focused on these targets. -
Pan-RAF Inhibitor
SJ-C1044 is a pan-RAF inhibitor that demonstrates both immunomodulatory and anti-tumor properties. This compound effectively targets wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values of 331, 257, and 187 nM, respectively, leading to inhibition of Kras activation and MEK-ERK phosphorylation, which reduces tumor cell proliferation. Additionally, SJ-C1044 exhibits inhibitory effects on VEGFR2, TIE2, and CSF1R, with IC50 values of 100, 23, and 235 nM, respectively, contributing to the improvement of the tumor immune microenvironment via the inhibition of angiogenesis and modulation of macrophage function. SJ-C1044 is suitable for research applications in colorectal cancer studies. -
BRAF/VEGFR2 Inhibitor
Takeda-6D is a potent and orally active inhibitor targeting BRAF and VEGFR2, displaying IC50 values of 7.0 nM and 2.2 nM, respectively. This compound effectively suppresses angiogenesis by inhibiting the VEGFR2 signaling pathway in 293/KDR and VEGF-stimulated HUVEC cells. Additionally, Takeda-6D demonstrates significant inhibition of ERK1/2 phosphorylation, indicating its potential for antitumor activity in various cancer research applications. -
SRC/Raf/VEGFR2 Inhibitor
SKLB646 is a multi-target kinase inhibitor with a focus on SRC, Raf, and VEGFR2. It exhibits potent inhibitory activity against SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively, as well as significant effects on B-Raf and C-Raf. SKLB646 disrupts SRC signaling and inhibits the MAPK pathway by targeting Raf kinases, leading to decreased proliferation, migration, and invasion in human umbilical vein endothelial cells (HUVEC), thereby impeding tumor-induced angiogenesis. It also demonstrates significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines, making it a valuable tool for cancer research. -
RET/BRAF/S6K/Src Inhibitor
AD57 is an orally active multikinase inhibitor that targets RET, BRAF, S6K, and Src, effectively reducing mTOR activity. This compound demonstrates significant biological activity by interfering with critical signaling pathways involved in cancer proliferation and survival. AD57 is suitable for research applications focused on cancer biology and therapeutic development against malignancies driven by these kinases. -
RET/BRAF/S6K/Src Inhibitor
AD57 hydrochloride is a multikinase inhibitor that targets RET, BRAF, S6K, and Src pathways. This orally active compound demonstrates significant biological activity in modulating aberrant signaling pathways associated with various cancers. Research applications include studying the effects of combined inhibition on tumor growth and resistance mechanisms in cancer cell lines and animal models. -
BRAF PROTACs Negative Control
CG 858-Neg is a negative control for Thalidomide-derived PROTAC degraders targeting BRAF and BRAFV600E, exhibiting Ki values of 9.5 nM and 14.4 nM, respectively. This compound effectively inhibits downstream phosphorylation of ERK and demonstrates suppression of BRAFV600E-driven tumorigenesis in melanoma (A375 cells, IC50 = 492 nM) and colorectal cancer (HT-29 cells, IC50 = 459 nM) models. CG 858-Neg is suitable for research applications focused on the mechanisms of melanoma and colorectal carcinoma. -
hRKIP-Raf1 Inhibitor
Cefotetan is a selective inhibitor of the human Raf1 kinase inhibitor protein (hRKIP). By binding to hRKIP, Cefotetan reduces its interaction with Raf1 kinase, thereby alleviating the inhibition of the Ras/Raf1/MEK/ERK signaling pathway and facilitating enhanced ERK phosphorylation. This mechanism makes Cefotetan valuable for research on diseases linked to dysregulated signaling within this pathway. Additionally, Cefotetan functions as a broad-spectrum antibacterial agent by binding to bacterial penicillin-binding proteins (PBPs) and disrupting cell wall synthesis, making it useful for investigating bacterial infections, particularly in the contexts of bone, skin, urinary tract, and lower respiratory tract infections. -
BRAF Kinase Inhibitor
Tinlorafenib is a potent inhibitor of BRAF and CRAF kinases, exhibiting IC50 values of 5.8 nM and 4.1 nM, respectively. It specifically targets V600E and V600K mutations in BRAF with IC50s of 4.25 nM and 2.7 nM, making it valuable for studying BRAF-driven tumors. Notably, Tinlorafenib demonstrates effective penetration of the blood-brain barrier, facilitating research into both central nervous system tumors and extracranial malignancies associated with BRAF mutations. -
RAF Molecular Glue
NST-628 is a molecular glue targeting RAF within the MAPK signaling pathway. It disrupts RAF phosphorylation and MEK activation by preventing the formation of BRAF-CRAF and BRAF-ARAF heterodimers. NST-628 exhibits significant biological activity in inhibiting RAS- and RAF-driven cancers, particularly in tumors with mutant KRAS, NRAS, BRAF class II/III, and NF1 mutations. This compound is a valuable tool for research into targeted cancer therapies and understanding the RAS-MAPK pathway's role in oncogenesis. -
pan-RAF Inhibitor
Exarafenib is a selective pan-RAF inhibitor that is available for oral administration. It is effective in targeting RAF-dependent cancers, specifically those with various BRAF alterations, by suppressing MAPK signaling pathways. Exarafenib has demonstrated significant anticancer activity in preclinical studies, making it a valuable tool for research in oncology and potential therapeutic applications in melanoma and other RAF-driven malignancies. -
BRAF Inhibitor
Claturafenib is a potent, orally active pan-mutant BRAF inhibitor. It effectively inhibits phosphorylated ERK (pERK) in cells, demonstrating an IC50 value of 1.6 nM in HT29 cell lines. Claturafenib exhibits significant antitumor activity against non-small cell lung cancer (NSCLC) harboring the BRAFG469A mutation and melanoma with the BRAFK601E mutation, making it a valuable tool for cancer research focused on BRAF mutant pathways. -
BRAF Inhibitor
Mosperafenib is a selective BRAF inhibitor designed to target BRAF V600 mutations. It exhibits significant biological activity against BRAF-mutant solid tumors, including colorectal cancer (CRC). This reagent is used in various research applications, particularly in the study of malignancies driven by BRAF mutations, enabling investigations into disease mechanisms and therapeutic strategies. -
RAF Inhibitor
TBAP-001 is a pan-RAF kinase inhibitor that targets the RAF signaling pathway. It exhibits potent inhibitory activity with an IC50 of 62 nM in the BRAF V600E kinase assay. This compound is utilized in research applications aimed at understanding the role of RAF kinases in cancer progression and therapeutic resistance, making it valuable for studies focused on targeted cancer therapies. -
B-Raf Inhibitor
B-Raf IN 11 is a selective inhibitor of the B-RafV600E mutant kinase, demonstrating an IC50 of 76 nM, and exhibits an IC50 of 238 nM against wild-type B-Raf kinase. This compound effectively inhibits the kinase activities of both B-RafV600E mutant and wild-type B-Raf, making it a valuable tool for investigating pathways related to colorectal cancer. Its application in research provides insight into therapeutic strategies targeting B-Raf mutations in cancer treatment. -
Raf Inhibitor
Flezurafenibum is a Raf kinase inhibitor that demonstrates significant antineoplastic activity. By selectively targeting the Raf pathway, it interferes with tumor growth and proliferation. This compound is of particular interest in cancer research, especially for studies involving Raf-mediated signaling pathways and potential therapeutic applications in various malignancies. -
BRAF Inhibitor
Uplarafenib is a selective BRAF inhibitor with an IC50 ranging from 50 to 100 nM. This compound displays significant antitumor activity, making it a valuable tool in cancer research. Uplarafenib is primarily utilized in studies investigating BRAF mutations and their role in tumorigenesis. -
BRAF Inhibitor
Braftide is an allosteric inhibitor of BRAF kinase that targets the dimer interface, effectively preventing the formation of BRAF dimers. It exhibits inhibitory activity against both wild-type BRAF and the oncogenic variant BRAFG469A, with IC50 values of 364 nM and 172 nM, respectively. By inhibiting the MAPK signaling pathway, Braftide demonstrates the ability to suppress the proliferation of KRAS mutant tumor cells, with EC50 values of 7.1 µM and 6.6 µM for HCT116 and HCT-15 cell lines, respectively. This compound is applicable in various cancer research studies. -
BRAF Inhibitor
B-Raf IN 15 is a potent BRAF inhibitor that selectively targets both BRAF wild-type and BRAF V600E variants, exhibiting IC50 values of 2.0 μM and 0.8 μM, respectively. This compound is particularly valuable in cancer research, facilitating studies on the pathways involved in tumor growth and progression. B-Raf IN 15 serves as an effective tool for evaluating therapeutic strategies and understanding the mechanisms of BRAF-related malignancies. -
RAF Inhibitor
PLX7922 is a selective RAF inhibitor that targets BRAFV600E mutations. It effectively inhibits phosphorylated ERK (pERK) in BRAFV600E cell lines, while paradoxically activating pERK in NRAS mutant cell lines. This compound is valuable for studying the signaling pathways involved in cancer, particularly in the context of RAS/RAF/MEK/ERK pathway alterations. -
RAS/RAS-RAF Inhibitor
RAS/RAS-RAF-IN-1 is a potent inhibitor targeting the RAS and RAS-RAF signaling pathways. With a dissociation constant (KD) in the range of 5.0 μM to 15 μM for cyclophilin A (CYPA), this compound demonstrates significant binding affinity. RAS/RAS-RAF-IN-1 exhibits notable antitumor activity, making it a valuable tool for cancer research and therapeutic development. -
RAF Inhibitor
GNE-9815 is a highly selective pan-RAF inhibitor that targets both CRAF and BRAF with Ki values of 0.062 nM and 0.19 nM, respectively. It demonstrates good oral bioavailability and, when used in conjunction with MEK inhibitors such as Cobimetinib, leads to synergistic modulation of the MAPK pathway. GNE-9815 is particularly useful in research focused on KRAS mutant cancers, facilitating the exploration of therapeutic strategies in this context. -
BRAF Inhibitor
Vem-L-Cy5 is a BRAF inhibitor that incorporates the near-infrared fluorophore cyanine-5 (Cy5). This compound specifically targets the BRAFV600E mutation and effectively inhibits MEK phosphorylation. Vem-L-Cy5 demonstrates cell permeability and has been shown to inhibit the growth of various cancer cell types, making it a valuable tool for cancer research and therapeutic development. -
b/cRAF Inhibitor
SHR902275 is a selective and potent b/cRAF inhibitor, specifically designed to target RAS mutant cancers. It demonstrates impressive inhibitory activity with IC50 values of 1.6 nM for cRAF, 10 nM for bRAFwt, and 5.7 nM for the bRAFV600E mutation. In cellular assays, SHR902275 effectively inhibits growth with GI50 values of 1.5 nM and 0.17 nM for H358, as well as 0.4 nM and 0.32 nM for A375 and Calu6, and SK-MEL2 cells, respectively. This compound holds potential for research applications focused on targeted cancer therapies and understanding RAF signaling pathways. -
Raf Inhibitor
Belvarafenib TFA is a potent pan-RAF inhibitor that targets the rapidly accelerated fibrosarcoma (RAF) family of kinases. It demonstrates impressive inhibitory activity, with IC50 values of 56 nM for B-RAF, 7 nM for B-RAFV600E, and 5 nM for C-RAF. This compound is valuable for research focusing on cancer therapeutics, particularly for the treatment of tumors driven by aberrant RAF signaling pathways. -
Raf Inhibitor
Brimarafenib is a selective inhibitor of Raf kinase, primarily targeting the MAPK/ERK signaling pathway. It exhibits significant antineoplastic activity, making it valuable for cancer research, specifically in the study of tumors driven by aberrant Raf signaling. Brimarafenib is utilized in preclinical models to investigate its therapeutic potential and mechanisms of action in various malignancies. -
Ras-Raf Inhibitor
Cyclorasin 9A5 is an 11-residue cyclic peptide that acts as an orthosteric inhibitor of the Ras-Raf protein interaction, exhibiting an IC50 of 120 nM. This compound is valuable for studying the Ras signaling pathway's involvement in various cancers and cellular processes. Its cell-permeable nature allows for effective in vitro and in vivo applications in cancer research and drug development targeting Ras-dependent pathways. -
c-Raf Inhibitor
(Z)-GW 5074 is a selective c-Raf inhibitor that demonstrates unique interactions with mutant huntingtin protein (mHTT) and LC3, without affecting wild-type huntingtin protein. This compound effectively inhibits c-Raf signaling, playing a crucial role in cellular responses associated with neurodegenerative disorders. (Z)-GW 5074 is primarily utilized in research focused on neurodegeneration and related biochemical pathways, providing valuable insights into therapeutic strategies targeting these diseases.
