Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11158 |
EGFR-IN-11
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-11 是 EGFR-酪氨酸激酶的选择性抑制剂,可诱导细胞凋亡。 EGFR-IN-11 抑制三重突变体 EGFRL858R/T790M/C797S,IC50 为 18 nM,并在 G0/G1 时阻止细胞周期。 | |||
T63528 | HSP90-IN-11 | ||
HSP90-IN-11 是 HSP90 的有效抑制剂,诱导亚 G1 期群体的显着积累。 HSP90-IN-11 具有与 AUY-922 (Luminespib) 相当的有效 HSP90α 抑制作用。在 CRC 和 NSCLC 细胞中,HSP90-IN-11 具有显着的抗增殖活性,在两位数 nM 范围内。HSP90-IN-11 能够快速降解 NSCLC 细胞中客户蛋白 EGFR 和 Akt 。 | |||
T41155 |
MS 154
|
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MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioa... | |||
T35430 | Afatinib impurity 11 | ||
Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1]. [1]. Li D, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11. |