Chemical Structure : INCB126503
CAS No.:
2640089-88-7
INCB126503
(INCB-126503)
Catalog No.: PC-24894Not For Human Use, Lab Use Only.
INCB126503 is a highly potent, selective, orally bioavailable FGFR2/3 inhibitor with IC50 of 2.1/1.2 nM respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
INCB126503 is a highly potent, selective, orally bioavailable FGFR2/3 inhibitor with IC50 of 2.1/1.2 nM respectively.
INCB126503 shows potent activity when tested against both of the FGFR3 gatekeeper mutants FGFR3-V555L (IC50 = 0.92 nM) and FGFR3-V555 M (IC50 = 0.85 nM).
INCB126503 displays single-digit nanomolar potency against FGFR3 in BAF3 cells (IC50 = 6.8 nM) while featuring excellent selectivity over FGFR1 (58-fold), also is highly selective over FGFR4 (IC50 = 64 nM).
INCB126503 inhibits both pFGFR3 and pERK signaling in RT112/84 tumor cells following a single oral dose of 100 mg/kg in RT112/84 tumors, demonstrates significant antitumor efficacy without inducing hyperphosphatemia.
Physicochemical Properties
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M.Wt
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470.58
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Formula
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C27H30N6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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Pyrrolo[1,2-a]pyrazin-7-ol, 2-[5-[5-(2,3-dimethylphenyl)-6-methoxy-1H-pyrazolo[4,3-b]pyridin-3-yl]-2-pyridinyl]octahydro-, (7R,8aS)-
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References
1. Nguyen MH, et al. ACS Med Chem Lett. 2025 May 17;16(6):1182-1189.
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