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IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT).
IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT).
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 16,100 | 10-14周 | |
50 mg | ¥ 21,300 | 10-14周 | |
100 mg | ¥ 27,500 | 10-14周 |
产品描述 | IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT). |
靶点活性 | IDH1 (R132C):0.045 μM , IDH1 (WT):2.52 μM , IDH1 (R132H):0.021 μM |
体外活性 | IDH1 Inhibitor 1 inhibits cellular HCT116-IDH1R132H/+ with an IC50 of 0.039 μM. |
体内活性 | IDH1 Inhibitor 1 is also profiled in a patient-derived IDH1 mutant HCT116-IDH1R132H/+ mechanistic xenograft tumor model in mice to evaluate in vivo inhibition of 2-HG production. IDH1 Inhibitor 1, dosed orally at 150 mg/kg, inhibits new 2-HG production.IDH1 Inhibitor 1 ?inhibits 2-hydroxyglutarate (2-HG) production in a preclinical xenograft tumor model. |
分子量 | 450.39 |
分子式 | C20H18F4N6O2 |
CAS No. | 2234285-81-3 |
密度 | 1.31g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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