Catalog No.
Product Name
Application
Product Information
Citations
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CSF-1 receptor inhibitor
Edicotinib is a selective and orally available colony-stimulating factor-1 (CSF-1) receptor inhibitor, and has entered phase IIA clinical trial to study rheumatoid arthritis (RA) despite disease. -
EGFR inhibitor
CO-1686 is a novel, oral, targeted covalent (irreversible) inhibitor of the cancer-causing mutant forms of epidermal growth factor receptor (EGFR) currently being studied for the treatment of non-small cell lung cancer (NSCLC). -
EGFR inhibitor
Poziotinib is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.- Yuji Uehara, .et al. , Lung Cancer, 2025, Apr:202:108479 PMID: 40088581
- Ikei S Kobayashi, .et al. , Cells, 2021, 10(12): 3561 PMID: 34944068
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IGF-1R, Aurora, FGFR, ABL, SRC inhibitor
XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases. -
Chk2, KDR, FGFR, Aurora A & Cdk2 inhibitor
R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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EGFR inhibitor
CL-387785 is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level. -
FGFR1 inhibitor
SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 uM -
ALK Inhibitor
LDK378 is a highly selective, orally bioavailable and ATP-competitive small molecule inhibitor of ALK (Anaplastic Lymphoma Kinase), a receptor tyrosine kinase considered to be an important lung cancer drug target. -
ALK Inhibitor
Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.- Sang-Yun Lee, .et al. , J Exp Clin Cancer Res, 2023, Nov 22;42(1):309 PMID: 37993887
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CDK/JAK2/FLT3 inhibitor
SB1317 is a potent inhibitor of Cyclin dependent kinases (CDKs), FMS-like tyrosine kinase-3 (FLT3) and Janus kinase 2 (JAK2) with IC50 values of 13nM, 56nM and 73nM for CDK2, JAK2 and FLT3, respectively. -
Tie-2 inhibitor
AMG-Tie2-1 is a highly potent, non-selective inhibitor of Tie-2 (IC50 <1 nM). -
c-Abl/c-Kit/PDGRFβ inhibitor
Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 a and VEGF in U266 cell line in a time- and dose-dependent manners, so flumatinib mesylate may become a new drug for MM therapy. - PP1 Analog II, 1NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.
- Luca Takacs, .et al. , Cell Rep, 2025, Apr 22;44(4):115534 PMID: 40220295
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EGFR inhibitor
Tyrphostin AG 183 inhibits EGFR (epidermal growth factor receptor) tyrosine kinase (IC50 = 800 nM). -
EGFR Inhibitor
EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells. -
EGFR inhibitor
Osimertinib (AZD-9291) is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors.
- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Sang-Hyun Lee, .et al. , NPJ Precis Oncol, 2024, May 21;8(1):111 PMID: 38773241
- Liyanage Manosika Buddhini Perera, .et al. , Biol Pharm Bull, 2024, 47(4):750-757 PMID: 38556260
- Liu YN, .et al. , Int J Cancer, 2019, Jun 4 PMID: 31162839
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EGFR inhibitor
Icotinib hydrochloride is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R). -
TRK inhibitor
GNF-5837 is a potent, selective, and orally bioavailable pan-TRK inhibitor that inhibited tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF.- Tanimizu N, .et al. , Development, 2018, Apr 25;145(9). pii: dev159095 PMID: 29615468
- Shargh VH, .et al. , Nanomedicine (Lond), 2017, May;12(9):977-989 PMID: 28440712
- Shargh VH, .et al. , Int J Pharm, 2016, Dec 30;515(1-2):527-534 PMID: 27793712
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Axl Inhibitor
R428 is a selective small molecule inhibitor of Axl kinase, which showed activity to blocks tumor spread and prolongs survival in models of metastatic breast cancer.- Ofra Novoplansky, .et al. , J Exp Clin Cancer Res, 2024, Nov 20;43(1):308 PMID: 39567998
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EGFR inhibitor
CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer. -
Src inhibitor
PD 166285 is a potent inhibitor of the tyrosine kinases c-Src, Flg (fibroblast growth factor receptor 1, FGFR1).
