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UM-164
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。
UM-164图片
CAS NO:903564-48-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
DAS-DFGO-II
产品介绍
UM-164 (DAS-DFGO-II) 是一种高效的c-Src抑制剂,Kd为 2.7 nM。UM-164 还高效抑制p38αp38β活性。
生物活性

UM-164 (DAS-DFGO-II) is a highly potent inhibitor ofc-Srcwith aKdof 2.7 nM. UM-164 also potently inhibitsp38αandp38β.

IC50& Target[1]

c-Src

2.7 nM (Kd)

p38α

 

p38β

 

体外研究
(In Vitro)

In biochemical assays, UM-164 is a highly potent inhibitor of c-Src with a binding constant comparable with Dasatinib (UM-164 Kd=2.7 nM, Dasatinib Kd=0.7 nM). To confirm that UM-164 is capable of inhibiting the activation of c-Src in vitro, the effect of UM-164 is examined on the c-Src autophosphorylation in two TNBC cell lines (MDA-MB 231 and SUM 149). Inhibition of c-Src autophosphorylation is detected in a concentration- and a time-dependent manner. At 120 minutes, complete abrogation of c-Src autophosphorylation is observed at 50 nM, demonstrating that UM-164 is a potent c-Src inhibitor in vitro. Flow cytometry experiments demonstrate that UM-164 treatment of MDA-MB 231 and SUM 149 increased the proportion of G0-G1cells by 25% and 28%, respectively, and concurrently decreased the fraction of S cells by 16% and 19%, respectively[1].

体内研究
(In Vivo)

A xenograft study is performed using NCr/nude mice implanted with MDA-MB 231 and SUM 149 cell lines. Once the tumors become palpable, the mice are randomized into control and treatment groups. Mice are injected intraperitoneally with either drug (10 and 20 mg/kg in both xenograft studies; a 15 mg/kg dose is added to the SUM 149 xenograft studies) or vehicle every other day (n=5 for each group). At the selected doses of UM-164, there is no significant weight loss or gross abnormalities observed in the treated animals, even after 52 days of treatment. However, tumor growth is significantly inhibited in both the 10 mg/kg and 20 mg/kg dose groups compared with the vehicle-treated group (P<0.026 and P<0.004, respectively)[1].

分子量

640.68

性状

Solid

Formula

C30H31F3N8O3S

CAS 号

903564-48-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL(7.80 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.5608 mL7.8042 mL15.6084 mL
5 mM0.3122 mL1.5608 mL3.1217 mL
10 mM---------
*

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。