S80359 |
Ivosidenib |
源葉(MedMol) | 99% |
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- 產(chǎn)品描述: Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity
- 靶點(diǎn): 12 nM (mouse IDH1R132H);Dehydrogenase;IsocitrateDehydrogenase(IDH)
- 體外研究:
Ivosidenib (AG-120) (0-13 μM; 48 hours) inhibits several IDH1-R132 mutants with potency similar IC50 values: IDH1-R132H (IC50=12 nM); IDH1-R132C (IC50=13 nM); IDH1-R132G (IC50=8 nM); IDH1-R132L (IC50=13 nM); IDH1-R132S (IC50=12 nM), respectively
- 體內(nèi)研究:
AG-120 (gavage administration; 50 mg/kg and 150 mg/kg) declines tumor 2-HG concentration rapidly, with maximum inhibition (92.0% and 95.2% at the 50 mg/kg and 150 mg/kg doses, respectively) achieved at -12 h post dose. Animal Model: Female nude BALB/c mice inoculated with HT1080 cells Dosage: 50 mg/kg and 150 mg/kg Administration: Gavage administration; 50 mg/kg and 150 mg/kg Result: Showed robust tumor 2-HG reduction in mouse.
- 參考文獻(xiàn):
1. Popovici-Muller J, et al. Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1Mutant Cancers. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305.
- 溶解性: soluble in DMSO
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.715 ml 8.577 ml 17.154 ml 5 mM 0.343 ml 1.715 ml 3.431 ml 10 mM 0.172 ml 0.858 ml 1.715 ml 50 mM 0.034 ml 0.172 ml 0.343 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)