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DS-1001b

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Chemical Structure| 1898207-64-1 同义名 : DS-1001
CAS号 : 1898207-64-1
货号 : A1213617
分子式 : C29H29Cl3FN3O4
纯度 : 99%+
分子量 : 608.916
MDL号 : MFCD32263044
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(49.27 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.64mL

0.33mL

0.16mL

8.21mL

1.64mL

0.82mL

16.42mL

3.28mL

1.64mL
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