产品
编 号：F747295
分子式：C28H28FN5O3
分子量：501.55
分子式：C28H28FN5O3
分子量：501.55
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 1816272-18-0
产品详情
生物活性：
(S,R)-GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values 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)-GSK321 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)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers.
体内研究：
(S,R)-GSK321 (150 mg/kg; i.p.; daily, for 15 d; male CD-1 mice with IDH1 mutant AML xenograft) reduces leukemic blasts in vivo.Animal Model:Male CD-1 mice with IDH1 mutant AML xenograft
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 (SSClowCD45low/+) and a relative increase in mature lymphoid and granulocytic/monocytic cells.
体外研究：
(S,R)-GSK321 (0.1-10000 nM; 24 h) inhibits intracellular 2-HG production in HT1080 cells with an EC50 value of 85 nM.(S,R)-GSK321 (0-5 μM; 48 h; HT1080 fibrosarcoma cells) leads to reduction of histone H3K9 dimethylation (H3K9me2).(S,R)-GSK321 (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).(S,R)-GSK321 (3 μM; 15 d) affects proliferation of primary IDH1 mutant AML cells.(S,R)-GSK321 (3 μM; 9 d) induces differentiation in primary IDH1 mutant AML blasts and immature stem-like cells.
(S,R)-GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values 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)-GSK321 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)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers.
体内研究：
(S,R)-GSK321 (150 mg/kg; i.p.; daily, for 15 d; male CD-1 mice with IDH1 mutant AML xenograft) reduces leukemic blasts in vivo.Animal Model:Male CD-1 mice with IDH1 mutant AML xenograft
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 (SSClowCD45low/+) and a relative increase in mature lymphoid and granulocytic/monocytic cells.
体外研究：
(S,R)-GSK321 (0.1-10000 nM; 24 h) inhibits intracellular 2-HG production in HT1080 cells with an EC50 value of 85 nM.(S,R)-GSK321 (0-5 μM; 48 h; HT1080 fibrosarcoma cells) leads to reduction of histone H3K9 dimethylation (H3K9me2).(S,R)-GSK321 (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).(S,R)-GSK321 (3 μM; 15 d) affects proliferation of primary IDH1 mutant AML cells.(S,R)-GSK321 (3 μM; 9 d) induces differentiation in primary IDH1 mutant AML blasts and immature stem-like cells.
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