XY0206 | FLT3 inhibitor | Probechem Biochemicals

Chemical Structure : XY0206

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XY0206 (XY-0206)

货号: PC-27991Not For Human Use, Lab Use Only.

XY0206 is a potent and oral FMS-like tyrosine kinase 3 (FLT3) inhibitor with IC50 of 0.7 nM, 5.27 nM and 6.92 nM for FLT3-ITD, FLT3 and RET, suppresses downstream STAT5, AKT, and ERK signaling, resulting in apoptosis in FLT3-ITD AML cells.

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生物&药学活性

XY0206 is a potent and oral FMS-like tyrosine kinase 3 (FLT3) inhibitor with IC50 of 0.7 nM, 5.27 nM and 6.92 nM for FLT3-ITD, FLT3 and RET, suppresses downstream STAT5, AKT, and ERK signaling, resulting in apoptosis in FLT3-ITD AML cells.
XY0206 strongly inhibits FLT3, along with other RTKs including RET and PDGFRβ (IC50=26 nM), inhibits PDGFRα, KDR, KIT, and ALK with IC50 of 158-675 nM.
XY0206 exhibits preferential anti-leukemic activity in FLT3-ITD-mutated AML cells with IC50 of 5.88 nM, 14.97 nM, and 4.35 nM for MV4-11, MOLM13, and Ba/F3-FLT3-ITD.
XY0206 retains activity against FLT3-ITD AML cells harboring the FLT3-F691L gatekeeper mutation.
XY0206 retains activity in FLT3-ITD AML with growth factor-associated and acquired resistance.
XY0206 demonstrates anti-leukemic activity with favorable tolerability in patient-derived AML blasts and preclinical mouse models.

物理化学性质&存储条件

分子量	404.87
分子式	C20H22ClFN4O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S,Z)-N-(5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrol-3-yl)pyrrolidine-2-carboxamide hydrochloride

参考文献

1. Shen L, et al. J Clin Invest. 2026 Sep 1:e204701.

XY0206 (XY-0206)

生物&药学活性

物理化学性质&存储条件

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XY0206 (XY-0206)

生物&药学活性

物理化学性质&存储条件

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