Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11157L |
EGFR-IN-1 hydrochloride
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-1 hydrochloride 是 L858R/T790M 突变体 EGFR 的不可逆特异性抑制剂,选择性是野生型 EGFR 的 100 倍。 EGFR-IN-1 hydrochloride 在 H1975 细胞和突变体 HCC827 细胞中表现出有效的抗肿瘤和抗增殖活性,IC50 分别为 4 和 28 nM。 | |||
T75261 | EGFR-IN-1 TFA | ||
EGFR-IN-1 TFA 是一种口服活性不可逆的突变型选择性 L858R/T790MEGFR 抑制剂。与野生型 EGFR 相比,EGFR-IN-1 TFA 对 Gefitinib 耐药的 EGFRL858R/T790M 有 100 倍的抑制作用。EGFR-IN-1 TFA 对 H1975 细胞和 HCC827 细胞具有较强的抗增殖活性。具有抗肿瘤活性。 | |||
T11157 |
EGFR-IN-1
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-1, an orally active and irreversible selective inhibitor targeting L858R/T790M mutant EGFR, exhibits strong antiproliferative and antitumor activity, particularly against H1975 cells and first line mutant HCC827 cells. This compound potently inhibits Gefitinib-resistant EGFR L858R/T790M mutations with a 100-fold selectivity over the wild-type EGFR. |