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XY0206

Chemical Structure : XY0206

CAS No.: 2057439-31-1

XY0206 (XY-0206)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 404.87
Formula C20H22ClFN4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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