GDC-0339|cas:1428569-85-0|西域试剂

GDC-0339,99.77%

产品编号：Bellancom-16976| CAS NO：1428569-85-0| 分子式：C₂₀H₂₂F₃N₇OS| 分子量：465.50

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货号	价格	库存与货期
Bellancom-16976	￥5000.00	杭州北京（现货）
Bellancom-16976	￥8000.00	杭州北京（现货）
Bellancom-16976	￥26000.00	杭州北京（现货）
Bellancom-16976	￥45000.00	杭州北京（现货）

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GDC-0339

产品介绍

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 K_i 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。

生物活性

GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with K_is 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.

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

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

西域 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
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.

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.

西域 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
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.

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.

西域 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
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.

性状

Solid

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式