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FGFR

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Cat. No. Product Name Field of Application Chemical Structure
DC11931 Alofanib Featured Alofanib ((RPT-835) is a potent, selective, allosteric FGFR2 inhibitor that significantly inhibits bFGF-induced proliferation of HUVEC cells with IC50 of 11 nM
DC1075 AZD4547 Featured AZD4547 is a novel selective FGFR inhibitor targeting FGFR1, FGFR2, and FGFR3 with IC50 of of 0.2 nM, 2.5 nM, and 1.8 nM, respectively.
DC5194 NVP-BGJ398(Infigratinib) Featured BGJ398 (NVP-BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.
DC10092 BLU554(Fisogatinib) Featured BLU-554 is a potent fibroblast growth factor receptor 4 (FGFR4) inhibitor.
DC8280 BLU-9931 Featured BLU9931 is the first selective small molecule inhibitor of FGFR4 with IC50 of 3 nM; less potent for FGFR1/2/3(IC50> 150 nM).
DC8418 CH5183284 (Debio-1347) Featured CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.
DC10559 Derazantinib (ARQ 087) Featured Derazantinib (Derazantinib) is an ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
DC4157 Dovitinib (TKI258, CHIR258) Featured Dovitinib (TKI258, CHIR258) is a novel multi-target inhibitor for Flt3, c-Kit, FGFR1/3, VEGFR1/2/3, PDGFRα/β with IC50 of 1 nM, 2 nM, 8 nM/9 nM and 10 nM/13 nM/8 nM, 210 nM/27 nM respectively.
DC10313 Dovitinib lactate Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.
DC11387 Erdafitinib Featured Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1-4 with IC50 values of 1.2, 2.5, 3.0 and 5.7nM, respectively.
DC10128 FGF401( Roblitinib) Featured FGF401 is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity.
DC9933 FGFR4-IN-1 FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.
DC8330 FIIN-2 Featured FIIN-2 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor.
DC9642 FIIN-3 Featured FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor.
DC10033 H3B-6527 Featured H3B-6527 is an orally bioavailable inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity.
DC7019 LY-2874455 Featured LY2874455 is a novel and potent FGF/FGFR inhibitor.
DC9945 NSC-12 NSC12 is a PTX3-derived anti-FGF small molecule, inhibits FGF-dependent tumor growth, angiogenesis, and metastases,acts as a small-molecule FGF trap in cancer therapy.
DC10068 PD166866 Featured PD-166866 is a selective inhibitor of the FGF-1 receptor tyrosine kinase (FGFR1) with IC50 = 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.
DC2054 PD-173074 Featured PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM.
DC10641 PRN1371 Featured PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively.
DC7508 SU 5402 Featured SU5402（SU-5402; SU5402） is 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).
DC10271 SUN11602 Featured SUN11602 is a novel aniline compound, which mimics the neuroprotective mechanisms of basic fibroblast growth factor.
DC11089 TAS-120 (Futibatinib) Featured TAS-120 is a highly potent and selective irreversible FGFR inhibitor, effective in tumors harboring various FGFR gene abnormalities.
DC28032 EMI1 (EGFR MaMTH Inhibitor 1) Featured EMI1 (EGFR MaMTH Inhibitor 1) is a novel EGFR ex19del/T790M/C797S inhibitor.EMI1, while potently reducing the interaction of EGFR triple mutant with Shc1 in our MaMTH-DS assay, did not behave as a TKI and displayed no inhibition of the kinase activity of EGFR triple-mutant protein invitro.EMI1 did, however, more strongly inhibit the viability and increase the caspase 3/7 activ-ity of PC9 EGFR ex19del/T790M/C797S triple-mutant cells than noncancerous human bronchial epithelial (HBE) cells, as well as potently reduce PC9 EGFR ex19del/T790M/C797S organ-oid viability.EMI1 had a similar inhibi-tory effect on microtubule plus-end growth in both EGFR-WT and EGFR-C797S triple-mutant cells at 50–100 nM concentration. At 1 µM concentration, EMI1 strongly depolymerized inter-phase microtubules, perturbed spindle formation and induced strong mitotic block in PC9 EGFR ex19del/T790M/C797S cells after 20 h of treatment. EMI1 inhibited interaction of both proteins with EGFR at a level similar to that observed with Shc1, indicating it is not a specific inhibitor of the EGFR-Shc1 PPI interface. Rather, the loss of interaction mediated by EMI1 appears to be due to a more general alteration in EGFR activity.EMI1 induced EGFR degradation, and inhibited the activation of EGFR, ERK, AKT and S6 in PC9-ex19del and PC9-ex19del/T790M cells.
DC28557 FGFR4-IN-4 FGFR4-IN-4 (compound 693) is a FGFR4 inhibitor with anti-tumor activity, extracted from patent WO2018113584A1.
DC40209 ZUN97585(FGFR1/DDR2 inhibitor 1) Featured FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.
DC42424 CPL304110 Featured CPL304110 is a potent, orally active and selective of fibroblast growth factor receptors FGFR (1-3), with IC50 values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively.
DC45315 SU4984 SU4984 is a protein tyrosine kinase inhibitor, with an IC50 of 10-20 μM for fibroblast growth factor receptor 1 (FGFR1). SU4984 is also inhibits platelet-derived growth factor receptor, and insulin receptor. SU4984 can be used for the research of cancer.
DC46449 FGFR1 inhibitor-2 FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer.
DC46931 Gunagratinib Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer.
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