货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S83260-1mg	≥98%	￥1890.00 S83260-1mg ￥1890.00 3-5天	0 货期：3-5天	-	-	-	-
S83260-5mg	≥98%	￥4990.00 S83260-5mg ￥4990.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S83260-1mg

≥98%

￥1890.00

货期：3-5天

S83260-5mg

≥98%

￥4990.00

货期：3-5天

产品描述：

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

靶点：

Ki: 0.03 nM (Pim1), 0.1 nM (Pim2), 0.02 nM (Pim3);Pim

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.

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.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.148 ml	10.741 ml	21.482 ml
5 mM	0.43 ml	2.148 ml	4.296 ml
10 mM	0.215 ml	1.074 ml	2.148 ml
50 mM	0.043 ml	0.215 ml	0.43 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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