| Identification | Back Directory | [Name]
ERLOTINIB MESYLATE | [CAS]
248594-19-6 | [Synonyms]
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 | [Molecular Formula]
C23H27N3O7S | [MDL Number]
MFCD08272810 | [MOL File]
248594-19-6.mol | [Molecular Weight]
489.54 |
| Hazard Information | Back Directory | [Uses]
Erlotinib mesylate (CP-358774 mesylate) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib (mesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [in vivo]
There is a 1.49-fold statistically significant difference between AUC0-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)[3]. 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[4]. | [IC 50]
EGFR: 2 nM (IC50) | [References]
[1] Moyer JD, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 1997 Nov 1;57(21):4838-48. PMID:9354447
[2] Ali S, et al. Apoptosis-inducing effect of erlotinib is potentiated by 3,3'-diindolylmethane in vitro and in vivo using an orthotopic model of pancreatic cancer. Mol Cancer Ther, 2008, 7(6), 1708-1719. DOI:10.1158/1535-7163.MCT-08-0354
[3] Marchetti S, et al. Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice.Mol Cancer Ther. 2008 Aug;7(8):2280-7. DOI:10.1158/1535-7163.MCT-07-2250
[4] Adachi K, et al. Effects of erlotinib on lung injury induced by intratracheal administration of bleomycin (BLM) in rats. J Toxicol Sci. 2010 Aug;35(4):503-14. DOI:10.2131/jts.35.503 |
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