Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5168 |
EGFR-IN-12
EGFR Inhibitor |
Apoptosis; EGFR | Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-12 (EGFR Inhibitor) 是一种 4,6-二取代的嘧啶,可诱导细胞凋亡,具有抗肿瘤活性。它是ATP 竞争性,不可逆且高度选择性的EGFR 抑制剂,IC50为 21 nM。它对EGFR 的选择性高于 HER4 和 55种其他激酶。它还抑制突变型EGFRL858R 和EGFRL861Q,IC50分别为 63 nM 和 4 nM。 | |||
T12131 | Mutated EGFR-IN-3 | EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Mutated EGFR-IN-3 is a ATP-competitive and highly selective allosteric dibenzodiazepinone EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) inhibitor(IC50 of 12 nM and 13 nM, respectively. ) | |||
T36648 | Tucatinib hemiethanolate | ||
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ... | |||
T35897 |
ASK120067
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ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT... |