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CAS No.: 1898207-64-1

DS-1001b Catalog No. CSN25248

Synonyms: DS-1001B;DS-1001

DS-1001b is a novel selective mutant IDH1 inhibitor with antitumor activity.

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生物活性

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技术信息

生物活性

描述Heterozygous mutations in genes encoding isocitrate dehydrogenase (IDH) 1 and 2 are frequently detected in acute myeloid leukemia (AML), angioimmunoblastic T-cell lymphoma, glioma, and cholangiocarcinoma. Mutant IDH catalyzes the formation of the oncometabolite D-2-hydroxyglutarate (D-2-HG). DS-1001b, a novel, orally bioavailable, selective mutant IDH1 inhibitor, impaired the proliferation of chondrosarcoma cells with IDH1 mutations in vitro and in vivo, and decreased 2-HG levels. Exposure to 1 μM DS-1001b for 72 h markedly decreased intracellular 2-HG levels in JJ012 and L835 cells. Intracellular D-2-HG levels were 100-fold higher than L-2-HG levels and completely blocked with 1 μM DS-1001b for 72 h in both IDH1-mutated cell lines. DS-1001b (0 - 10 μM) impaired proliferation in both cell lines in a dose-dependent manner. It decreased cell viability in a dose-dependent manner even under 3D and hypoxic conditions. Furthermore, treatment with different concentrations of DS-1001b for 72 h decreased intracellular 2-HG levels in a dose-dependent manner in JJ012 and L835 cells. In vivo, continuous administration of DS-1001b significantly impaired subcutaneous tumor growth in JJ012 xenograft mice. Moreover, 2-HG levels were markedly lower in DS-1001b-treated mice than in untreated mice (P < 0.001)^[1].
参考文献

[1] Nakagawa M, Nakatani F, Matsunaga H, et al. Selective inhibition of mutant IDH1 by DS-1001b ameliorates aberrant histone modifications and impairs tumor activity in chondrosarcoma. Oncogene. 2019;38(42):6835-6849

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
- 1.6423 mL
- 8.2113 mL
- 16.4226 mL
- 5 mM
- 0.3285 mL
- 1.6423 mL
- 3.2845 mL
- 10 mM
- 0.1642 mL
- 0.8211 mL
- 1.6423 mL

技术信息

CAS号

1898207-64-1

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H29Cl3FN3O4

运输

蓝冰

分子量

608.92

别名

DS-1001B;DS-1001

溶解度

DMSO	14.0 mg/mL (23.0 mM)
Water	Insoluble
Ethanol	Insoluble

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