1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)
  3. (S,R)-GSK321

(S,R)-GSK321 是一个有效的选择性突变型 IDH1 抑制剂,抑制 R132G、R132C、R132H 和 WT IDH1IC50 值分别为 2.9、3.8、4.6 和 46 nM,选择性比 IDH2 高出 100 倍。(S,R)-GSK321 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)-GSK321 可用于急性髓系白血病 (AML) 及其他癌症的研究。

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(S,R)-GSK321 Chemical Structure

(S,R)-GSK321 Chemical Structure

CAS No. : 1816272-18-0

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Other Forms of (S,R)-GSK321:

查看 Isocitrate Dehydrogenase (IDH) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

IDH1

 

体外研究
(In Vitro)

(S,R)-GSK321 (0.1-10000 nM; 24 h) inhibits intracellular 2-HG production in HT1080 cells with an EC50 value of 85 nM[1].
(S,R)-GSK321 (0-5 μM; 48 h; HT1080 fibrosarcoma cells) leads to reduction of histone H3K9 dimethylation (H3K9me2)[1].
(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)[1].
(S,R)-GSK321 (3 μM; 15 d) affects proliferation of primary IDH1 mutant AML cells[1].
(S,R)-GSK321 (3 μM; 9 d) induces differentiation in primary IDH1 mutant AML blasts and immature stem-like cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
体内研究
(In Vivo)

(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 (SSClowCD45low/+) and a relative increase in mature lymphoid and granulocytic/monocytic cells.
分子量

501.55

Formula

C28H28FN5O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (199.38 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9938 mL 9.9691 mL 19.9382 mL
5 mM 0.3988 mL 1.9938 mL 3.9876 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9938 mL 9.9691 mL 19.9382 mL 49.8455 mL
5 mM 0.3988 mL 1.9938 mL 3.9876 mL 9.9691 mL
10 mM 0.1994 mL 0.9969 mL 1.9938 mL 4.9845 mL
15 mM 0.1329 mL 0.6646 mL 1.3292 mL 3.3230 mL
20 mM 0.0997 mL 0.4985 mL 0.9969 mL 2.4923 mL
25 mM 0.0798 mL 0.3988 mL 0.7975 mL 1.9938 mL
30 mM 0.0665 mL 0.3323 mL 0.6646 mL 1.6615 mL
40 mM 0.0498 mL 0.2492 mL 0.4985 mL 1.2461 mL
50 mM 0.0399 mL 0.1994 mL 0.3988 mL 0.9969 mL
60 mM 0.0332 mL 0.1662 mL 0.3323 mL 0.8308 mL
80 mM 0.0249 mL 0.1246 mL 0.2492 mL 0.6231 mL
100 mM 0.0199 mL 0.0997 mL 0.1994 mL 0.4985 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
(S,R)-GSK321
目录号:
HY-128888B
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