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CHMFL-EGFR-202 是一种有效、不可逆的表皮生长因子受体 (EGFR) 突变型激酶抑制剂, 对耐药突变型 EGFR T790M 和 WT EGFR 激酶作用的 IC50 分别为 5.3 nM 和 8.3 nM。


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CHMFL-EGFR-202 是一种有效、不可逆的表皮生长因子受体 (EGFR) 突变型激酶抑制剂, 对耐药突变型 EGFR T790M 和 WT EGFR 激酶作用的 IC50 分别为 5.3 nM 和 8.3 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 774 | In Stock | |
| 2 mg | ¥ 1,150 | In Stock | |
| 5 mg | ¥ 1,790 | In Stock | |
| 10 mg | ¥ 2,630 | In Stock | |
| 25 mg | ¥ 4,140 | In Stock | |
| 50 mg | ¥ 5,680 | In Stock | |
| 100 mg | ¥ 7,680 | In Stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 1,980 | In Stock |
CHMFL-EGFR-202 相关产品
| 产品描述 | CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase (IC50s: 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases). |
| 靶点活性 | BMX?kinase:111 nM, EGFR (T790M):5.3 nM, ErbB2:8.1 nM, EGFR:8.3 nM, MEK1:161 nM, BLK:8.1 nM, BTK:24.5 nM, ERB4:3.2 nM |
| 体外活性 | CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 potently inhibits EGFR primary mutants (L858R, del19) and drug-resistant mutant L858R/T790M. CHMFL-EGFR-202 displays strong binding affinities against wild-type, L861Q, G719C/S, L858R/T790M, L858R, and T790M among EGFR wild-type and mutant kinases. CHMFL-EGFR-202 also exhibits strong binding affinities against BLK, BMX, BTK, ERBB2, ERBB4, LOK, MEK1, and MEK5 kinases (percent of control score less than 1% at 1 μM). CHMFL-EGFR-202 strongly inhibits BLK, BTK, ERBB2 and ERBB4 (IC50s: of 8.1 nM, 24.5 nM, 8.1 nM and 3.2 nM). CHMFL-EGFR-202 moderately inhibits BMX and MEK1 kinases (IC50s: 111.0 nM and 161.0 nM)[1]. |
| 分子量 | 489.96 |
| 分子式 | C25H24ClN7O2 |
| CAS No. | 2089381-40-6 |
| Smiles | NC1=C2C(=NN(C2=NC=N1)[C@H]3CN(C(C=C)=O)CCC3)C4=CC(Cl)=C(OCC5=CC=CC=N5)C=C4 |
| 密度 | no data available |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 45 mg/mL (91.84 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.08 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||
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DMSO
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