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CAS No.: 1448346-63-1

AG-120（外消旋） Catalog No. CSN19720

Synonyms: Ivosidenib Racemate;AG-120;RG-120 (racemic)

AG-120 Racemate is the racemate form of AG-120 with no activity.

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技术信息

生物活性

描述Isocitrate dehydrogenases (IDHs) catalyze the oxidative decarboxylation of isocitrate to 2-oxoglutarate. IDH1 is a NADP(+)-dependent isocitrate dehydrogenase found in the cytoplasm and peroxisomes. IDH1 serves a significant role in cytoplasmic NADPH production. Somatic mutations in IDH1 have recently been identified in multiple human cancers. Mutation at the site of R132 of IDH1 confer on this enzymes a new activity: catalysis of alpha-ketoglutarate (2-OG) to the (R)-enantiomer of 2-hydroxyglutarate (R-2HG). AG-120 Racemate is the racemate form of AG-120. AG-120 is a selective inhibitor of R132 mutated IDH1. The inhibitory IC₅₀s of AG-120 against IDH1-R132 mutants IDH1-R132H, IDH1-R132C, IDH1-R132G, IDH1-R132L and IDH1-R132S were 12, 13, 8, 13, and 12 nM, respectively. The inhibitory IC₅₀s of AG-120 against IDH1-R132 mutated HT1080, COR-L105 and HCCC-9810 cells were 8, 15 and 12 nM, respectively^[3]. In IDH1-R132 mutated samples derived from AML patients, AG-120 reduced the level of intracellular 2-HG by 96% at the lowest tested dose (0.5 μM) and by 98.6% and 99.7%, respectively, at 1 and 5 μM. 5 μM AG-120 also enhanced ability of primary patient myeloblasts to form differentiated colonies in methylcellulose assays^[3]. In HT1080 xenografts established in nude mice, a single oral dose of AG-120 at 50 or 150 mg/kg reduced tumor 2-HG concentration with maximum inhibition of 92.0% and 95.2%, respectively, achieved at about 12h post dose^[3].
参考文献

[1] WO2015127172A1
[2] WO2015138839A1
[3] Popovici-Muller J, Lemieux RM, Artin E, Saunders JO, Salituro FG, Travins J, Cianchetta G, Cai Z, Zhou D, Cui D, Chen P, Straley K, Tobin E, Wang F, David MD, Penard-Lacronique V, Quivoron C, Saada V, de Botton S, Gross S, Dang L, Yang H, Utley L, Chen Y, Kim H, Jin S, Gu Z, Yao G, Luo Z, Lv X, Fang C, Yan L, Olaharski A, Silverman L, Biller S, Su SM, Yen K. Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7154 mL
- 8.5769 mL
- 17.1538 mL
- 5 mM
- 0.3431 mL
- 1.7154 mL
- 3.4308 mL
- 10 mM
- 0.1715 mL
- 0.8577 mL
- 1.7154 mL

技术信息

CAS号

1448346-63-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H22ClF3N6O3

运输

蓝冰

分子量

582.96

别名

Ivosidenib Racemate;AG-120;RG-120 (racemic);RG-120;Ivosidenib (racemic)

溶解度

DMSO	100.0 mg/mL (171.5 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (171.5 mM)

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AG-120（外消旋） Catalog No. CSN19720

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