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EGFRL858R和EGFRL861Q，IC50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) |
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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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(604.74 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.4190 mL | 12.0948 mL | 24.1896 mL | | 5 mM | 0.4838 mL | 2.4190 mL | 4.8379 mL | | 10 mM | 0.2419 mL | 1.2095 mL | 2.4190 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。 |
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