Product Name :
Erlotinib Hydrochloride
Description:
Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM.
CAS:
183319-69-9
Molecular Weight:
429.90
Formula:
C22H24ClN3O4
Chemical Name:
N-(3-ethynylphenyl)-6, 7-bis(2-methoxyethoxy)quinazolin-4-amine hydrochloride
Smiles :
Cl.COCCOC1=CC2=NC=NC(NC3=CC(=CC=C3)C#C)=C2C=C1OCCOC
InChiKey:
GTTBEUCJPZQMDZ-UHFFFAOYSA-N
InChi :
InChI=1S/C22H23N3O4.ClH/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22;/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25);1H
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM.|Product information|CAS Number: 183319-69-9|Molecular Weight: 429.90|Formula: C22H24ClN3O4|Synonym:|CP-358774|CP358774|OSI-774|OSI 774|OSI774|Tarceva|CP-358, 774|Related CAS Number:|183321-74-6 (Erlotinib free base)|248594-19-6 (Erlotinib mesylate)|Chemical Name: N-(3-ethynylphenyl)-6, 7-bis(2-methoxyethoxy)quinazolin-4-amine hydrochloride|Smiles: Cl.COCCOC1=CC2=NC=NC(NC3=CC(=CC=C3)C#C)=C2C=C1OCCOC|InChiKey: GTTBEUCJPZQMDZ-UHFFFAOYSA-N|InChi: InChI=1S/C22H23N3O4.ClH/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22;/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25);1H|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO: 4 mg/mLwarmed(9.3 mM).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi humancolon cancer cells andMDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi humancolon cancer cells. Erlotinib inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM.{{Brassicasterol} site|{Brassicasterol} Inhibitor|{Brassicasterol} NF-κB|{Brassicasterol} Biological Activity|{Brassicasterol} Purity|{Brassicasterol} supplier} Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells.{{Mitotane} medchemexpress|{Mitotane} Apoptosis|{Mitotane} Technical Information|{Mitotane} Description|{Mitotane} supplier|{Mitotane} Epigenetic Reader Domain} The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells.PMID:28630660 Ten micromolar of Erlotinib HCl inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition.|In Vivo:|At doses of 100 mg/kg, Erlotinib HCl completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate.|References:|Moyer JD, et al. Cancer Res. 1997, 57(21), 4838-4848.Li T, et al. Clin Cancer Res, 2007, 13(11), 3413-3422.Ali S, et al. Mol Cancer Ther, 2008, 7(6), 1708-1719.Buck E, et al. Mol Cancer Ther. 2006, 5(11), 2676-2784.Higgins B, et al. Anticancer Drugs. 2004, (5), 503-512.Furugaki K,et al. Oncol Lett. 2010, 1(2), 231-235.Bago-Horvath Z, et al. 2012, DOI: 10.1159/000337257Products are for research use only. Not for human use.|