1. PI3K/Akt/mTOR
  2. PI3K
  3. GS-9901

GS-9901 是高度选择性的、口服有效的 PI3Kδ 的抑制剂,其 IC50 值为 1 nM。有用于风湿性关节炎的潜能。

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GS-9901 Chemical Structure

GS-9901 Chemical Structure

CAS No. : 1640247-87-5

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5 mg ¥2500
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10 mg ¥4200
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25 mg ¥9000
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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis[1].

IC50 & Target

PI3Kδ

1 nM (IC50)

体内研究
(In Vivo)

GS-9901 (0.3/1/3 mg/kg, orally, twice daily for 7 days) demonstrates efficacy in a rat model of arthritis and is predicted to be suitable for q.d. dosing in humans[1].

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

Animal Model: Female Lewis rats with established collagen-induced arthritis (CIA)[1].
Dosage: 0.3 mg/kg, 1 mg/kg, and 3 mg/kg.
Administration: Orally, twice-daily for 7 days starting on the 10th day after the second collagen immunization.
Result: Demonstrated significant reduction in ankle swelling in rats treated with 0.3 mg/kg 35 (31% reduction), 1 mg/kg 35 (67%), and 3 mg/kg 35 (65%).
Plasma concentrations measured on day 7 (12 h after last dose) were consistent with maintaining approximately 60%, 80%, and >90% inhibition of PI3Kδ at 0.3, 1.0, and 3 mg/kg doses, respectively, at trough levels.
分子量

477.88

Formula

C22H17ClFN9O

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 250 mg/mL (523.14 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0926 mL 10.4629 mL 20.9258 mL
5 mM 0.4185 mL 2.0926 mL 4.1852 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

GS-9901 相关分类

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 2.0926 mL 10.4629 mL 20.9258 mL 52.3144 mL
5 mM 0.4185 mL 2.0926 mL 4.1852 mL 10.4629 mL
10 mM 0.2093 mL 1.0463 mL 2.0926 mL 5.2314 mL
15 mM 0.1395 mL 0.6975 mL 1.3951 mL 3.4876 mL
20 mM 0.1046 mL 0.5231 mL 1.0463 mL 2.6157 mL
25 mM 0.0837 mL 0.4185 mL 0.8370 mL 2.0926 mL
30 mM 0.0698 mL 0.3488 mL 0.6975 mL 1.7438 mL
40 mM 0.0523 mL 0.2616 mL 0.5231 mL 1.3079 mL
50 mM 0.0419 mL 0.2093 mL 0.4185 mL 1.0463 mL
60 mM 0.0349 mL 0.1744 mL 0.3488 mL 0.8719 mL
80 mM 0.0262 mL 0.1308 mL 0.2616 mL 0.6539 mL
100 mM 0.0209 mL 0.1046 mL 0.2093 mL 0.5231 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:
GS-9901
目录号:
HY-100694
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