IDH-305 - IDH1(R132) 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIDH-305Cat. No.: HY-104036CAS No.: 1628805-46-8分式: CHFNO分量: 490.45作靶点: Isocitrate Dehydrogenase (IDH)作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL

2、(305.84 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0389 mL 10.1947 mL 20.3894 mL5 mM 0.4078 mL 2.0389 mL 4.0779 mL10 mM 0.2039 mL 1.0195 mL 2.0389 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实

3、验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.10 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.10 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.

4、MedChemEBIOLOGICAL ACTIVITY物活性 IDH-305种服性、突变选择性和脑渗透性的 IDH1 抑制剂，靶向 IDH1 (R132) 突变。IDH-305 对突变体IDH1 亚型的选择性野型 200 倍 (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 M (IDH1WT)。IC50 & Target IC50: 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 M (IDH1WT) 1体外研究 IDH-305 inhibits HCT116-IDH1R132H+/- cells wit

5、h an IC50 of 24 nM 1.体内研究 IDH-305 (30-300 mg/kg; p.o.; twice daily for 21 days) inhibits 2-HG production and 2-HG-dependent tumorgrowth of an IDH1 mutant PDX melanoma model 1.Animal Model: nu/nu mice (HMEX2838-IDH1R132C+/-PDX model) 1Dosage: 30, 100, 300 mg/kgAdministration: Oral gavage; twice daily

6、 for 21 daysResult: Resulted in 62-67% 2-HG reduction and significant anti-tumor activity at 100 mg/kg and97-99% 2-HG reduction and partial tumor regression of 32% at 300 mg/kg.REFERENCES1. Cho YS, et al. Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor.

7、 ACS Med Chem Lett.2017 Sep 18;8(10):1116-1121.2. Courtney D DiNardo, et al. A Phase I Study of IDH305 in Patients with Advanced Malignancies Including Relapsed/Refractory AML andMDS That Harbor IDH1R132 Mutations. Blood, 128(22), 1073.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use