GDC-0339 - CAS:1428569-85-0

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GDC-0339

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

Data Sheet 产品使用指南

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。

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10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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.

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

•Cell Chem Biol. 2021 Sep 8;S2451-9456(21)00400-1.

纯度： 98%

Data Sheet

产品使用指南

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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