1. JAK/STAT Signaling
  2. Pim
  3. GDC-0339

GDC-0339 是一种高效、具有口服活性、耐受性良好的 pan-Pim 激酶抑制剂,对 Pim1、Pim2 和 Pim3 作用的 Ki 值分别为 0.03 nM、0.1 nM 和 0.02 nM。GDC-0339 具有研究多发性骨髓瘤的潜力。

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GDC-0339 Chemical Structure

GDC-0339 Chemical Structure

CAS No. : 1428569-85-0

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5121
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1 mg ¥1904
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5 mg ¥5000
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10 mg ¥8000
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50 mg   询价  
100 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma[1][2].

IC50 & Target

PIM1

 

PIM2

 

PIM3

 

体外研究
(In Vitro)

GDC-0339 is cytostatic, with an IC50 of 0.1 μM for MM.1S cells[2].
GDC-0339 treatment reveals a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases[2].

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

Cell Viability Assay[2]

Cell Line: MM.1S cells
Concentration:
Incubation Time: 3 days
Result: Inhibited cell viability.

Western Blot Analysis[2]

Cell Line: MM.1S cells
Concentration: 0.01 μM, 0.03 μM, 0.09 μM,0.27 μM, 0.83 μM, 2.5 μM
Incubation Time: 4 hours
Result: Induced a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases.
体内研究
(In Vivo)

GDC-0339 (1-300 mg/kg; p.o; daily; for 21 days) is efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models[2].
GDC-0339 has a half-life of t1/2=0.9 h[2].

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

Animal Model: Female C.B-17 SCID mice, RPMI8226 human multiple myeloma xenograft mouse model[2]
Dosage: 1mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg, 300 mg/kg
Administration: Oral administration; once daily; for 21 days
Result: Showed dose-dependent tumor growth inhibition.
分子量

465.50

Formula

C20H22F3N7OS

CAS 号
性状

固体

颜色

White to yellow

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 52 mg/mL (111.71 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 2.1482 mL 10.7411 mL 21.4823 mL
5 mM 0.4296 mL 2.1482 mL 4.2965 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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

纯度: 99.77%

参考文献

GDC-0339 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1482 mL 10.7411 mL 21.4823 mL 53.7057 mL
5 mM 0.4296 mL 2.1482 mL 4.2965 mL 10.7411 mL
10 mM 0.2148 mL 1.0741 mL 2.1482 mL 5.3706 mL
15 mM 0.1432 mL 0.7161 mL 1.4322 mL 3.5804 mL
20 mM 0.1074 mL 0.5371 mL 1.0741 mL 2.6853 mL
25 mM 0.0859 mL 0.4296 mL 0.8593 mL 2.1482 mL
30 mM 0.0716 mL 0.3580 mL 0.7161 mL 1.7902 mL
40 mM 0.0537 mL 0.2685 mL 0.5371 mL 1.3426 mL
50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0741 mL
60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8951 mL
80 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.6713 mL
100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5371 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:
GDC-0339
目录号:
HY-16976
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