GDC-0339

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GDC-0339  纯度: 99.77%

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。

GDC-0339

GDC-0339 Chemical Structure

CAS No. : 1428569-85-0

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5 mg ￥5000 In-stock
10 mg ￥8000 In-stock
50 mg ￥26000 In-stock
100 mg ￥45000 In-stock
200 mg   询价  
500 mg   询价  

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GDC-0339 相关产品

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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[1][2].

IC50 & Target

Ki: 0.03 nM (Pim1), 0.1 nM (Pim2), 0.02 nM (Pim3)[2]
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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 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

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。
参考文献

  • [1]. Takahashi RH, et al. CYP1A1-Mediated Intramolecular Rearrangement of Aminoazepane in GDC-0339. Drug Metab Dispos. 2017 Oct;45(10):1084-1092.

    [2]. Wang X, et al. Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. J Med Chem. 2019 Feb 28;62(4):2140-2153.

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