HMPL-306 | IDH1/2 inhibitor | Probechem Biochemicals

Chemical Structure : HMPL-306

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HMPL-306 (Ranosidenib)

货号: PC-24264Not For Human Use, Lab Use Only.

规格	价格	库存	数量
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250 mg		Get quote

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生物&药学活性

HMPL-306 (Ranosidenib) is a potent, selective dual inhibitor of isocitrate dehydrogenase IDH1 and IDH2 with cell IC50 of 50/31/26 nM for U87MG IDH1-R132H/TF1 IDH1-R132H/ HT1080 (IDH1-R132C), respectively.
HMPL-306 (Ranosidenib) shows excellent selectivity against SafetyScreen panel at CEREP.
HMPL-306 (Ranosidenib) at 25 mg/kg demonstrated robust and sustained 2-HG inhibition in tumors, with inhibitory rates reaching 96%, 98% and 93% at 16, 24, and 40 h post dosing, respectively.
HMPL-306 (Ranosidenib) also displayed potent and durable mutant IDH1 inhibitory activity in fibrosarcoma HT1080 model harboring IDH1 R132C mutation.
HMPL-306 (Ranosidenib) demonstrated better brain penetration in mice.
HMPL-306 (Ranosidenib) showed good PK and safety profiles and reduced 2-HG in vivo robustly and sustainably in the mutant IDH1 and 2 tumor xenograft models.

物理化学性质&存储条件

分子量	453.31
分子式	C15H16F9N5O
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)-3-(4,6-bis(((R)-1,1,1-trifluoropropan-2-yl)amino)-1,3,5-triazin-2-yl)-2,6,6-trifluorocyclohex-2-en-1-ol

参考文献

1. Xiao K, et al. ACS Med Chem Lett. 2025 Feb 13;16(3):454-463.

HMPL-306 (Ranosidenib)

生物&药学活性

物理化学性质&存储条件

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HMPL-306 (Ranosidenib)

生物&药学活性

物理化学性质&存储条件

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