- Cat. No.
- A10080
Ponatinib (AP24534)
Synonyms: AP24534
AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.
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Fibroblast growth factor receptor (FGFR) inhibitors act on FGFR1 to FGFR4, four receptor tyrosine kinases. FGFR signaling controls cell proliferation, migration and differentiation in development and angiogenesis. Amplifications, activating mutations and gene fusions of FGFR genes have been found in many tumor types. PD173074 was crystallized with the FGFR1 kinase domain in 1998, which showed how it occupies the adenosine triphosphate (ATP) pocket. Infigratinib and fexagratinib are FGFR-focused inhibitors used to study cells that depend on FGFR signaling. Nintedanib and pazopanib HCl inhibit FGFR together with vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptors (PDGFRs). Kinases outside the FGFR family are covered by sibling categories such as VEGFR and PDGFR.
Synonyms: AP24534
AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.
Synonyms: GW786034
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.
Synonyms: BGJ-398
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).
Synonyms: Vargatef; Bibf1120
BIBF1120 (Vargatef) is a novel triple angiokinase inhibitor that inhibits three growth factor receptors simultaneously: VEGFR, PDGF and FGFR.
Synonyms: GW 786034; Votrient
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.
Synonyms: BMS-540215
Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.
Synonyms: TSU68; SU6668
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.
Synonyms: AZD-4547
Fexagratinib (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.
Synonyms: BIBF-1120 esylate
Nintedanib is a potent inhibitor of multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs).
PD173074 is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR.
Synonyms: PHA-739358
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
Synonyms: CHIR-258; TKI258
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.
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).
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.
FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor.
Synonyms: TAS-120
Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor.
Synonyms: BMS-582664
Brivanib alaninate (BMS-582664) is a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling.
Synonyms: CHIR-258; TKI258 Dilactic acid; CHIR-258 dilactic acid
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.
KW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
LY2874455 is a novel and potent FGFR/VEGFR Inhibitor.
MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.
Synonyms: Tyrosine kinase-IN-1
Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
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.
Synonyms: SSR
SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 uM