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248594-19-6

中文名稱 甲磺酸厄洛替尼
英文名稱 ERLOTINIB MESYLATE
CAS 248594-19-6
分子式 C23H27N3O7S
分子量 489.54
MOL 文件 248594-19-6.mol
248594-19-6 結(jié)構(gòu)式 248594-19-6 結(jié)構(gòu)式

基本信息

中文別名
甲磺酸厄洛替尼
埃羅替尼甲磺酸鹽
英文別名
ERLOTINIB MESYLATE
Erlotinib (OSI-744) mesylate
Erlotinib mesylate (CP-358774
CP-358774
OSI-774
NSC 718781
R 1415
TARCEVA
CP-358774
OSI-774
NSC 718781
R 1415
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度25℃: DMSO
形態(tài)粉末

常見問題列表

生物活性
Erlotinib mesylate (CP-358774 mesylate) 為 EGFR 抑制劑,IC50 值為 2 nM。
靶點(diǎn)

EGFR

2 nM (IC 50 )

體外研究

Erlotinib mesylate (CP-358774 mesylate) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC 50 of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC 50 of 100 nM for an 8-day proliferation assay. The combination of B-DIM and Erlotinib (2 μM) results in a significant inhibition of colony formation in BxPC-3 cells when compared with either agent alone. The combination of B-DIM and Erlotinib (2 μM) results in a significant induction of apoptosis only in BxPC-3 cells when compare with the apoptotic effect of either agent alone.

體內(nèi)研究

There is a 1.49-fold statistically significant difference between AUC 0-inf after p.o. administration of Erlotinib (5 mg/kg) comparing Bcrp1/Mdr1a/1b -/- and WT mice (7,419±1,720 versus 4,957±1,735 ng*h/mL respectively, P=0.01). The administration of Erlotinib (10 mg/kg/day, or 20 mg/kg/day) to Bleomycin (BLM)-treated rats shows no exacerbation of lung injuries in indices such as macroscopic findings, lung weights, histopathological scores (lung lesion density and lung fibrosis score), and pulmonary hydroxyproline (HyP) level. The result suggests that Erlotinib does not have any exacerbating effects on lung injuries induced by BLM in rats.

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