IDH-305
产品编号: DC10538
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应用领域
IDH-305 是一种口服性、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 亚型的选择性比野生型高 200 倍 (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 µM (IDH1WT))。
| Cas No.: |
1628805-46-8 |
| 名称: |
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| 别名: |
IDH-305,IDH 305,IDH305 |
| SMILES: |
O=C1OC[C@H]([C@@H](F)C)N1C2=NC(N[C@H](C3=CC(C)=C(C4=CC(C(F)(F)F)=NC=C4)C=N3)C)=NC=C2 |
| 分子式: |
C23H22F4N6O2 |
| 分子量: |
490.46 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| In Vitro: |
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| References: |
IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity. Upon administration, IDH305 specifically inhibits IDH1(R132) mutant forms in the cytoplasm, which inhibits the formation of the oncometabolite 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1(R132)-expressing tumor cells. |
| Kinase Assay: |
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| Cell Assay: |
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| Animal Administration: |
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| References: |
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MSDS
COA
| LOT NO. |
DOWNLOAD |
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| 2018-0101 |
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