DD205-291

Chemical Structure : DD205-291

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货号: PC-23276Not For Human Use, Lab Use Only.

DD205-291 is a potent, selective and orally bioavailable PROTAC-based hematopoietic progenitor kinase 1 (HPK1, MAP4K1) degrader with DC50 of 8.8 nM.

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生物&药学活性

DD205-291 is a potent, selective and orally bioavailable PROTAC-based hematopoietic progenitor kinase 1 (HPK1, MAP4K1) degrader with DC50 of 8.8 nM.
DD205-291 showed a dose-dependent inhibition of SLP-76 phosphorylation and an induction of IL-2 and IFN-γ. DD205-291 exhibited good efficacy and a favorable safety profile in the MC38 model.
DD205-291 (0.5 mg/kg) in combination with anti-PD1 resulted in significant suppression with a TGI value of 91.0%.

物理化学性质&存储条件

分子量	775.23
分子式	C38H38ClF3N10O3
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	1-(2-chloro-5-(4-((1-(5-(7-(1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)-5H-pyrrolo[2,3-b]pyrazin-2-yl)pyridin-2-yl)piperidin-4-yl)methyl)piperidine-1-carbonyl)phenyl)dihydropyrimidine-2,4(1H,3H)-dione

参考文献

1. Zhimin Zhang, et al. J Med Chem. 2024 Oct 24. doi: 10.1021/acs.jmedchem.4c01906.

DD205-291

生物&药学活性

物理化学性质&存储条件

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DD205-291

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物理化学性质&存储条件

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