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Lazertinib
An irreversible inhibitor of mutant EGFRs
AZD9291(Osimertinib)
Erlotinib
An EGFR tyrosine kinase inhibitor
TAS6417
TAS6417 (CLN-081, TPC-064) is a novel EGFR inhibitor that targets EGFR exon 20 insertion mutations while sparing wild-type (WT) EGFR. IC50 values ranges from 1.1 ± 0.1 to 8.0 ± 1.1 nmol/L.
AV-412
A dual inhibitor of EGFR and HER2
Afatinib dimaleate
An inhibitor of EGFR and ErbB2
ZM 323881 HCl
A potent and selective VEGFR2 inhibitor
PD168393
An irreversible EGFR kinase inhibitor
BMS-599626 Hydrochloride
BMS-599626 Hydrochloride (AC480 Hydrochloride) 是一种选择性的口服生物可利用的 HER1 和 HER2 抑制剂,IC50 分别为 20 和 30 nM。 BMS-599626 Hydrochloride 对 HER4 (IC50=190 nM) 的效力降低约 8 倍,对 VEGFR2、c-Kit、Lck、MEK 的效力超过 100 倍。 BMS-599626 Hydrochloride 抑制肿瘤细胞增殖,并有可能增加肿瘤对放疗的反应。
Mutated EGFR-IN-1
Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
N-Desethyl Sunitinib
An active metabolite of sunitinib
Dovitinib (TKI258) Lactate
A multi-kinase inhibitor
Nazartinib mesylate
An inhibitor of mutant EGFR
Mutated EGFR-IN-2
Mutated EGFR-IN-2 (compound 91) 突变选择性的 EGFR 抑制剂,有效抑制单突变体 EGFR (T790M) 和双突变体 EGFR (包括 L858R/T790M (IC50=<1nM) 和 ex19del/T790M),并且可以抑制单一功能获得性突变 EGFR (包括 L858R 和 ex19del) 的活性。Mutated EGFR-IN-2 具有抗肿瘤活性。
RTC-5
RTC-5 是一种具有抗癌效力的优化吩噻嗪。RTC-5 显示针对 EGFR 驱动的癌症的异种移植模型的功效,其效果归因于 PI3K-AKT 和 RAS-ERK 信号传导的负调节。