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Chemical Structure : KIN-3248
Catalog No.: PC-21321Not For Human Use, Lab Use Only.
Resigratinib (KIN-3248) is a next-generation, irreversible, orally available, small molecule pan-FGFR inhibitor with IC50 of 3.9/5.3/9.7 nM for FGFR1/2/3, potently inhibits FGFR2 and FGFR3 gatekeeper, molecular brake, and activation loop mutations with IC50 of 5-20 nM.
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Resigratinib (KIN-3248) is a next-generation, irreversible, orally available, small molecule pan-FGFR inhibitor with IC50 of 3.9/5.3/9.7 nM for FGFR1/2/3, potently inhibits FGFR2 and FGFR3 gatekeeper, molecular brake, and activation loop mutations with IC50 of 5-20 nM.
Resigratinib (KIN-3248) exhibits low nanomolar biochemical potency against wild-type FGFR family members as well as mutants associated with resistance to FGFR inhibitors (IC50 3.9-24.1 nM).
Resigratinib (KIN-3248) is active in human FGFR2-PHGDH fusion-positive CCLP-1 and FGFR2-OPTN fusion-positive ICC13-7 cholangiocarcinoma cell lines engineered to express wild-type or clinically relevant gatekeeper, molecular brake, and activation loop mutant alleles (EC50=2.4-9.9 nM).
Resigratinib (KIN-3248) induces dose-dependent tumor growth inhibition and regressions in FGFR inhibitor-resistant, patient-derived gastric cancer and cholangiocarcinoma models harboring secondary FGFR2 kinase domain mutations.
Resigratinib (KIN-3248) is highly-selective, potent and broad-spectrum activity against mutations in both the FGFR2 and FGFR3 kinase domains- including gatekeeper, molecular brake, and activation loop alterations.
| M.Wt | 523.54 | |
| Formula | C26H27F2N7O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Aleksandra Franovic, et al. 2022 ASCO Gastrointestinal Cancers Symposium.
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