Mutant IDH1/NAMPT-IN-1

CAS: F: C30H29FN6O4 W: 556.59

Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of mutant isocitrate dehydrogenase 1 (mutant IDH1) (IC50=14.93

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Bioactivity	Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of mutant isocitrate dehydrogenase 1 (mutant IDH1) (IC50=14.93 nM) and nicotinamide phosphoribosyltransferase (NAMPT) (IC50=12.56 nM). Mutant IDH1/NAMPT-IN-1 can induce apoptosis. Mutant IDH1/NAMPT-IN-1 crosses the blood-brain barrier effectively[1].
Invitro	Mutant IDH1/NAMPT-IN-1 (0.5-2 μM; 48 h) 能够剂量依赖性地降低 U87 MG-IDH1R132H 细胞中的 2-HG 水平[1]。Mutant IDH1/NAMPT-IN-1 对 U87 MG 的抗增殖活性 IC50=1.26 μM (24 h), 0.77 μM (48 h), 0.42 μM (72 h)。对 U87 MG-IDH1R132H 的抗增殖活性 IC50=0.89 μM (24 h), 0.47 μM (48 h), 0.32 μM (72 h])][1]。Mutant IDH1/NAMPT-IN (0.5 μM; 6 h) 提高 U87 MG-IDH1R132H 细胞中 NAMPT 和 IDH1R132H 的热稳定性[1]。Mutant IDH1/NAMPT-IN-1 (0.1-2 μM; 48 h) 剂量依赖性地诱导 U87 MG-IDH1R132H 细胞的凋亡sup>[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Mutant IDH1/NAMPT-IN-1 相关抗体: Apoptosis Analysis[1] Cell Line:
In Vivo	Mutant IDH1/NAMPT-IN-1 (i.v.; 10-40 mg/kg; 每天两次，连续 35 天) 能以剂量依赖的方式抑制 BALB/c 裸鼠的肿瘤生长[1]。Mutant IDH1/NAMPT-IN-1 (i.v.;400 mg/kg; 单剂量) 在 ICR 小鼠中用药安全[1]。药代动力学分析[1] Route
Formula	C30H29FN6O4
Molar Mass	556.59
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Wen F, et al. Discovery of Novel Dual Inhibitors Targeting Mutant IDH1 and NAMPT for the Treatment of Glioma with IDH1Mutation. J Med Chem. 2024 Apr 23.

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