DS21150768 | HPK1/MAP4K1 inhibitor | Probechem Biochemicals

Chemical Structure : DS21150768

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DS21150768 (DS-21150768)

货号: PC-21340Not For Human Use, Lab Use Only.

DS21150768 is a potent selective and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with IC50 of 3.27 nM in cell-free HPK1 assays, binds to HPK1 with an affinity constant (KD) of 6.08 nM.

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生物&药学活性

DS21150768 is a potent selective and orally active hematopoietic progenitor kinase 1 (HPK1, MAP4K1) inhibitor with IC50 of 3.27 nM in cell-free HPK1 assays, binds to HPK1 with an affinity constant (KD) of 6.08 nM.
DS21150768 is selective against MAP4K family members HGK (MAP4K4) and MINK (MAP4K6), and cell-free kinase panel assay of 174 kinases.
DS21150768 inhibits the phosphorylation of SLP76 (pSLP76) induced by the stimulation in a concentration-dependent manner (IC50=61.9 nM) in Jurkat cells, induces enhanced TCR signaling and cytokine production in T cells.
DS21150768 (30 mg/kg, orally) induced significant elevation of IFN-γ levels in plasma and spleen, DS21150768 (100 mg/kg, orally) treatment results in significant increases of both IL-2 and IFN-γ in vivo.
DS21150768 monotherapy (100 mg/kg, orally administered once every 2 days) and the combination treatment with anti-PD1 significantly inhibits tumor growth in B16-BL6, CT26.WT, Pan02, and RM-1.

物理化学性质&存储条件

分子量	618.69
分子式	C36H32F2N6O2
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	N-(4-(6-amino-2',6'-dimethyl-[3,4'-bipyridin]-5-yl)phenyl)-4-(((3-fluorobicyclo[1.1.1]pentan-1-yl)methyl)amino)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide

参考文献

1. Genzui Setsu, et al. Eur J Pharmacol. 2023 Nov 7:176184.

DS21150768 (DS-21150768)

生物&药学活性

物理化学性质&存储条件

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DS21150768 (DS-21150768)

生物&药学活性

物理化学性质&存储条件

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