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Cat. No. Product Name Target Signaling Pathways
T63769 EGFR-IN-60

EGFR-IN-60 是一种有效的、口服具有活力的、安全的抗肿瘤剂。EGFR-IN-60 能够明显抑制 EGFRWT (IC50: 83 nM)、EGFRT790M (IC50: 26 nM)、EGFRL858R (IC50: 53 nM) 和 JAK3 (IC50: 69 nM)。EGFR-IN-60 能够抑制携带 EGFRT790M 突变的 H1975 细胞 (IC50: 1.32 μM) ,并抑制过表达 EGFRWT 的 A431 细胞 (IC50: 4.96 μM)。EGFR-IN-60 能够提高 Bax/Bcl-2 比率,进而诱导细胞凋亡诱导并导致细胞死亡。
T3506 Nazartinib

那扎替尼,EGF816,NVS-816

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Nazartinib (EGF816) 是一种共价、不可逆、突变选择性 EGFR 抑制剂,对激活 mt (L858R, ex19del) 和 T790M mt 具有纳摩尔抑制效力,在体外其选择性比野生型 (wt) EGFR60 倍。
T73101 EGFR-IN-25

EGFR-IN-25 是一种有效的EGFR 抑制剂,对 BaF3 细胞 (EGFR DEL19/T790M/C797S) 和 A431 细胞 (WT) 的IC50分别为 9 nM 和 60 nM。
T71184 ARQ-736

ARQ 736 is a potent and selective BRAF inhibitor. ARQ 736 is selectively potent in killing cancer cell lines harboring at least one mutated BRAF allele. BRAF mutations were detected in over 60% of melanomas and may account for a significant proportion of colon cancer patients whose tumors are resistant to anti-EGFR therapy. The B-Raf protein is a key signaling molecule in the mitogen activated protein kinase (MAPK) signaling pathway and has been implicated in the pathogenesis of a variety of ca...
T36643 PKI-166 hydrochloride

Potent EGFR-kinase inhibitor (IC50 = 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable. Bruns et al (2000) Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 60 2926 PMID:10850439 |Ulu et al (2013) Epidermal ...

化合物

EGFR-IN-60
Cat.No: T63769
Synonym:
Target:
Nazartinib
Cat.No: T3506
Synonym: 那扎替尼,EGF816,NVS-816
Target: EGFR
EGFR-IN-25
Cat.No: T73101
Synonym:
Target:
ARQ-736
Cat.No: T71184
Synonym:
Target:
PKI-166 hydrochloride
Cat.No: T36643
Synonym:
Target:
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