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EGFR-IN-12
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。
EGFR-IN-12图片
CAS NO:879127-07-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
EGFR-IN-12 是一种 4,6-二取代的嘧啶,是一种有效的,ATP 竞争性,不可逆且高度选择性的EGFR抑制剂,IC50为 21 nM。EGFR-IN-12 还抑制突变型EGFRL858REGFRL861QIC50分别为 63 nM 和 4 nM。EGFR-IN-12 对EGFR的选择性高于 HER4 (IC50= 7640 nM) 和 55种其他激酶。EGFR-IN-12 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。
生物活性

EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selectiveEGFRinhibitor with anIC50of 21 nM. EGFR-IN-12 also inhibits mutantEGFRL858RandEGFRL861QwithIC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity forEGFRover HER4 (IC50= 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cellsapoptosisand has antitumor activity[1][2].

IC50& Target[1]

EGFR (WT)

21 nM (IC50)

EGFRL858R

63 nM (IC50)

EGFRL861Q

4 nM (IC50)

HER4

7640 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-12 (EGFR inhibitor 324674; 0-2 μM; 48 hours; HT29 and SW480 cells) treatment efficiently induces apoptosis at lower concentrations[2].
EGFR-IN-12 (EGFR inhibitor 324674; 0-3 μM; 3 hours; HT29 and SW480 cells) treatment inhibits EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner[2].
EGFR-IN-12 (EGFR inhibitor 324674) inhibits HT29 and SW480 cell proliferation with with IC50s of 1.96 μM and 1.04 μM, respectively[2].
Pretreatment of cells with EGFR-IN-12 (compound 1; 10 μM) results in complete inhibition of wild-type receptor autophosphorylation in U-2OS cells. And the T766M mutant receptor is completely resistant to inhibition by EGFR-IN-12[1].

Apoptosis Analysis[1]

Cell Line:HT29 and SW480 cells
Concentration:0 μM, 1 μM, 2 μM
Incubation Time:48 hours
Result:Induced apoptosis in HT29 cells and SW480 cells.

Western Blot Analysis[1]

Cell Line:HT29 and SW480 cells
Concentration:0 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time:3 hours
Result:Inhibited EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner.
分子量

413.40

性状

Solid

Formula

C21H18F3N5O

CAS 号

879127-07-8

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 : 250 mg/mL(604.74 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4190 mL12.0948 mL24.1896 mL
5 mM0.4838 mL2.4190 mL4.8379 mL
10 mM0.2419 mL1.2095 mL2.4190 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。