(S,R)-WT IDH1 Inhibitor 2

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CAS NO:	1816272-18-0
包装:	10mg
市场价:	13050元

(S,R)-WT IDH1 Inhibitor 2 (GSK321) 是一个有效的选择性突变型 IDH1 抑制剂，抑制 R132G、R132C、R132H 和 WT IDH1 的 IC50 值分别为 2.9、3.8、4.6 和 46 nM，选择性比 IDH2 高出 100 倍。(S,R)-WT IDH1 Inhibitor 2 诱导细胞内 2-HG 减少，髓细胞分化阻滞失效，在白血病母细胞和更不成熟的干细胞水平诱导粒细胞分化。(S,R)-WT IDH1 Inhibitor 2 可用于急性髓系白血病 (AML) 及其他癌症的研究。

Cas No.

1816272-18-0

别名

GSK321

分子式

C₂₈H₂₈FN₅O₃

分子量

501.55

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

IC50: 2.9 (R132G), 3.8 (R132C), 4.6 (R132H) and 46 nM (WT IDH1)^[1]

(S,R)-WT IDH1 Inhibitor 2 (GSK321) is a potent, selective mutantIDH1inhibitor withIC₅₀values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-WT IDH1 Inhibitor 2 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-WT IDH1 Inhibitor 2 can be used for research of acute myeloid leukemia (AML) and other cancers^[1].

(S,R)-WT IDH1 Inhibitor 2 (GSK321; 0.1-10000 nM; 24 h) inhibits intracellular 2-HG production in HT1080 cells with an EC₅₀value of 85 nM^[1].
(S,R)-WT IDH1 Inhibitor 2 (0-5 μM; 48 h; HT1080 fibrosarcoma cells) leads to reduction of histone H3K9 dimethylation (H3K9me2)^[1].
(S,R)-WT IDH1 Inhibitor 2 (3 μM; 22 d) decreases intracellular 2-HG in a dose-dependent manner (R132G, 0.13-fold; R132C, 0.15-fold; R132H, 0.29-fold)^[1].
(S,R)-WT IDH1 Inhibitor 2 (3 μM; 15 d) affects proliferation of primary IDH1 mutant AML cells^[1].
(S,R)-WT IDH1 Inhibitor 2 (3 μM; 9 d) induces differentiation in primary IDH1 mutant AML blasts and immature stem-like cells^[1].

Cell Viability Assay^[1]

Cell Line:	IDH1 mutant AML cells
Concentration:	3 μM
Incubation Time:	15 days
Result:	Increased in cell numbers (2-fold to 15-fold) in IDH1 mutant AML cells.

Cell Cycle Analysis^[1]

Cell Line:	IDH1 mutant AML cells
Concentration:	3 μM
Incubation Time:	15 days
Result:	Decreased in quiescent (G0)-phase cells and increased in G1-phase in R132G IDH1.

Western Blot Analysis^[1]

Cell Line:	HT1080 fibrosarcoma cells
Concentration:	0, 0.5 and 5 μM
Incubation Time:	48 hours
Result:	Induced markedly decreased H3K9me2 levels.

(S,R)-WT IDH1 Inhibitor 2 (GSK321; 150 mg/kg; i.p.; daily, for 15 d; male CD-1 mice with IDH1 mutant AML xenograft) reduces leukemic blasts in vivo^[1].

Animal Model:	Male CD-1 mice with IDH1 mutant AML xenograft^[1]
Dosage:	150 mg/kg
Administration:	Intraperitoneal injection; daily, for 15 days
Result:	Decreased in 2HG in IDH1-mutant AML cells. Decreased in the percentage of blast cells (^SSClowCD45^low/+) and a relative increase in mature lymphoid and granulocytic/monocytic cells.