GW2974是EGFR和Neu（ErbB-2）受体酪氨酸激酶的双重选择性抑制剂。众所周知，酪氨酸激酶是跨膜蛋白，对细胞生长和存活至关重要。研究表明，GW2974通过抑制酪氨酸激酶的能力抑制癌症细胞系PC-3的生长。此外，GW2974刺激细胞中NSE和Chr-A（嗜铬粒蛋白A）的量。涉及BK5.erbB2小鼠的研究表明，GW2974抑制12-O-十四烷酰佛波醇-13-乙酸酯诱导的表皮过度增殖，导致EGFR和Neu的表达降低。此外，这些研究表明，在肿瘤促进和Neu过表达期间，GW2974对细胞生长的抑制作用更强。 GW2974 is a dual selective inhibitor of EGFR and Neu (ErbB-2) receptor tyrosine kinases. It is known that tyrosine kinases are transmembrane proteins, which are essential in cell growth and survival. Studies indicate that GW2974 inhibits cancer line PC-3 growth, via its ability to inhibit tyrosine kinases. In addition, GW2974 stimulates the amount of NSE and Chr-A (chromogranin A) in cells. Studies involving BK5.erbB2 mice show that GW2974 inhibits 12-O-tetradecanoylphorbol-13-acetate-induced epidermal hyperproliferation, which resulted in a lower expression of EGFR and Neu. Furthermore, these studies suggest that the inhibitory effects on cell growth of GW2974 is more potent during tumor promotion and when Neu is overexpressed.
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GW2974
Dangerous GoodsCAS number：202272-68-2 molecular formula：C23H21N7
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| Chinese alias | - | ||
| English alias | EGFR/HER2 Inhibitor | EU-0100509 | HMS3303J07 | SCHEMBL1737530 | J-013131 | NSC756204 | NSC-756204 | Q27167122 | DTXSID20220889 | LP00509 | N*4*-(1-Benzyl-1H-indazol-5-yl)-N*6*,N*6*-dimethyl-pyrido[3,4-d]pyrimidine-4,6-diamine | N6,N6-dimethyl-N4-[1-(phen | ||
| CAS number | 202272-68-2 | molecular formula | C23H21N7 |
| molecular weight | 395.46 g/mol | Exact mass | - |
| PSA | 71.800 Ų | logp | 4.000 |
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Safety information
WGK Germany：
3
Personal protective equipment：
Eyeshields， Gloves， type N95 (US)， type P1 (EN143) respirator filter
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