GDC-0339

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GDC-0339

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1428569-85-0

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

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 toleratedpan-Pim kinaseinhibitor, withK_is of 0.03 nM, 0.1 nM and 0.02 nM forPim1,Pim2andPim3, 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 IC₅₀of 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].

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].

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

性状

Solid

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。