GDC-0339
目录号 : KM11476 CAS No. : 1428569-85-0 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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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.

体外研究

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

Cell Viability Assay

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

Western Blot Analysis

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

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.
GDC-0339 has a half-life of t1/2=0.9 h.

Animal Model: Female C.B-17 SCID mice, RPMI8226 human multiple myeloma xenograft mouse model
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.
分子式
C20H22F3N7Os
分子量
465.50
CAS号
1428569-85-0
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
In Vitro: 

DMSO : ≥ 52 mg/mL (111.71 mM)

* "≥" 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
10 mM 0.2148 mL 1.0741 mL 2.1482 mL
*

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。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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