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Catalog No.
Product Name
Application
Product Information
Product Citation
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BCR-ABL inhibitor
AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Yamamoto Y, .et al. , Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- N Naganna, .et al. , EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Takuya Hirao, .et al. , Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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VEGFR inhibitor
BIBF1120 (Vargatef) is a novel triple angiokinase inhibitor that inhibits three growth factor receptors simultaneously: VEGFR, PDGF and FGFR.- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Chun-Jung Chang, .et al. , Biochem Pharmacol, 2021, Jan;183:114356 PMID: 33285108
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VEGFR inhibitor
Brivanib alaninate (BMS-582664) is a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling. -
RTK inhibitor
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively. -
VEGFR-2 inhibitor
Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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VEGFR/PDGFR/FGFR inhibitor
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Hideharu Yamada, .et al. , Oncol Lett, 2021, Jun;21(6):455 PMID: 33907565
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
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FGFR1/VEGFR2 Inhibitor
PD173074 is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR.- Cheryl Q.E. Lee, .et al. , Stem Cell Reports, 2016, Feb 9; 6(2): 257-272 PMID: 26862703
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Aurora inhibitor
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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PDFGRβ inhibitor
Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Aaron Y. Lai, .et al. , Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
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FGFR inhibitor
AZD4547 is a potent, selective and orally active pan-FGFR inhibitor, with IC50s of 0.2, 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively.- Ryuma Tokunaga, .et al. , Oncotarget, 2016, Apr 12; 7(15): 19748-19761 PMID: 26933914
- Mitsuko Kawano, .et al. , Adv Radiat Oncol, 2016, Jul-Sep; 1(3): 170-181 PMID: 28740887
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FGFR Inhibitor
BGJ398 is a potent and selective inhibitor with potential antiangiogenic and antineoplastic activities of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively).- Takehito Yamamoto, .et al. , Cancers (Basel), 2020, Jul 22;12(8):E2010 PMID: 32708005
- Daniel Limonta, .et al. , J Infect Dis, 2019, 2019 PMID: 30799482
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Anil Kumar, .et al. , Sci Rep, 2018, 8: 5477 PMID: 29615760
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RTK inhibitor
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.- Yunping Hu, .et al. , Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
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VEGFR inhibitor
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.- Koide H, .et al. , Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. , Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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VEGFR/FGFR/EGFR inhibitor?€?
SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively). -
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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FGFR1 inhibitor
SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 uM -
FGFR1/2/3 inhibitor
Debio-1347 is an orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity. -
FGFR Inhibitor
NVP-BGJ398 phosphate is a novel selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively; >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. -
FGFR2 Inhibitor
Alofanib is a potent and selective allosteric inhibitor of FGFR2 with potential anticancer activity. -
FGFR inhibitor
Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. -
RTK inhibitor
Nintedanib is a potent inhibitor of multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs).- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Thibaut Fourniols, .et al. , Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
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FGFR4 inhibitor
Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity. -
TACC3 inhibitor
KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3). -
multi-targeted kinase inhibitor
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively. -
FGFR3 inhibitor
Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM. -
tyrosine kinase inhibitor
Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM. -
VEGFR-2/FGFR inhibitor
CP-547632 hydrochloride is a well-tolerated, orally-bioavailable inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. -
FGFR1 inhibitor
Ferulic acid sodium is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively. -
FGFR inhibitor
2,5-Dihydroxybenzoic acid is a derivative of benzoic and a powerful inhibitor of fibroblast growth factors. -
FGFR3 inhibitor
VSPPLTLGQLLS is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation.
