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Erlotinib Hydrochloride

CAS No. : 183319-69-9

MCE 站：Erlotinib Hydrochloride

产品活性：Erlotinib Hydrochloride (CP-358774 Hydrochloride) 抑制 EGFR 激酶的 IC₅₀ 为 2 nM。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK  |  Autophagy

作用靶点：EGFR  |  Autophagy

In Vitro: Erlotinib Hydrochloride (CP-358774 Hydrochloride) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC₅₀ of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC₅₀ 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.

In Vivo: 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.

相关产品：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  CNS-Penetrant Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Differentiation Inducing Compound Library  |  Anti-COVID-19 Compound Library  |  NMPA-Approved Drug Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Hepatitis C Virus Compound Library  |  Anti-Lung Cancer Compound Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Targeted Therapy Drug Library   |  Gefitinib  |  Trastuzumab  |  Erlotinib  |  Cetuximab  |  AG490  |  Genistein  |  AG-1478  |  Pertuzumab  |  BI-4020  |  NSC 228155  |  Pelitinib  |  Mubritinib  |  TX1-85-1  |  Canertinib  |  Butein  |  PD168393  |  Daphnetin  |  EGFR-IN-7  |  AEE788  |  Chrysophanol  |  PD153035  |  Tyrphostin 23  |  Lavendustin A  |  Trastuzumab emtansine  |  BMS-599626 Hydrochloride  |  PD158780  |  AV-412

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