HM-279 | ALK5 inhibitor | Probechem Biochemicals

Chemical Structure : HM-279

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HM-279 (HM279)

货号: PC-24274Not For Human Use, Lab Use Only.

HM-279 is a potent, selective, orally bioavailable inhibitor of ALK5 (TGFβR1) with IC50 of 4.7 nM, strongly inhibits the phosphorylation of Smad3 in A549 cells (IC50=21.6 nM).

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生物&药学活性

HM-279 is a potent, selective, orally bioavailable inhibitor of ALK5 (TGFβR1) with IC50 of 4.7 nM, strongly inhibits the phosphorylation of Smad3 in A549 cells (IC50=21.6 nM).
HM-279 has fair to good selectivity against other TGF-β receptor family kinases, with 4.5–693-fold selectivity.
HM-279 induces antitumor activity through modulation of antitumor immunity rather than direct cytotoxicity to cancer cells.
HM-279 (p.o., 30 mg/kg, QD antitumor activity of HM-279 in nude mice or a CD8+ T cell depletion mouse model.

物理化学性质&存储条件

分子量	451.55
分子式	C22H25N7O2S
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	2-((1-(But-2-yn-1-yl)-1H-pyrazol-4-yl)(cyclopropylmethyl)amino)-5-(4-(dimethylcarbamoyl)-1H-pyrrol-2-yl)thiazole-4-carboxamide

参考文献

1. Arai M, et al. J Med Chem. 2025 Mar 19. doi: 10.1021/acs.jmedchem.4c02293.

HM-279 (HM279)

生物&药学活性

物理化学性质&存储条件

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HM-279 (HM279)

生物&药学活性

物理化学性质&存储条件

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