Erlotinib hydrochloride
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Category | Enzyme inhibitors |
Catalog number | BBF-04613 |
CAS | 183319-69-9 |
Molecular Weight | 429.90 |
Molecular Formula | C22H23N3O4.HCl |
Purity | >98% |
Ordering Information
Catalog Number | Size | Price | Stock | Quantity |
---|---|---|---|---|
BBF-04613 | 25 g | $199 | In stock |
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Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 = 20 nM), DiFi humancolon cancer cells and MDA MB-468 human breast cancer cells.
Specification
Related CAS | 183321-74-6 (free base) |
Synonyms | OSI-744; OSI744; OSI 744; Tarceva; 4-(m-Ethynylanilino)-6,7-bis(2-methoxyethoxy)quinazoline monohydrochloride; 6,7-bis(2-methoxyethoxy)-4-(3-ethynylanilino)quinazoline hydrochloride |
Storage | Store at 2-8°C |
IUPAC Name | N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine;hydrochloride |
Canonical SMILES | COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl |
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 |
InChI Key | GTTBEUCJPZQMDZ-UHFFFAOYSA-N |
Source | Synthetic |
Properties
Appearance | Off-white Solid |
Application | Antineoplastic Agents |
Boiling Point | 553.6°C at 760 mmHg |
Melting Point | 223-225°C |
Solubility | Soluble in Acetic Acid, Dimethylformamide, Dimethyl Sulfoxide, Methanol |
Reference Reading
1.Effect of Sulindac and Erlotinib vs Placebo on Duodenal Neoplasia in Familial Adenomatous Polyposis: A Randomized Clinical Trial.
Samadder NJ1, Neklason DW2, Boucher KM3, Byrne KR4, Kanth P4, Samowitz W5, Jones D6, Tavtigian SV6, Done MW7, Berry T7, Jasperson K7, Pappas L7, Smith L7, Sample D7, Davis R7, Topham MK8, Lynch P9, Strait E10, McKinnon W11, Burt RW12, Kuwada SK13. JAMA. 2016 Mar 22-29;315(12):1266-75. doi: 10.1001/jama.2016.2522.
IMPORTANCE: Patients with familial adenomatous polyposis (FAP) are at markedly increased risk for duodenal polyps and cancer. Surgical and endoscopic management of duodenal neoplasia is difficult and chemoprevention has not been successful.
2.Potential of erlotinib cyclodextrin nanosponge complex to enhance solubility, dissolution rate, in vitro cytotoxicity and oral bioavailability.
Dora CP1, Trotta F2, Kushwah V3, Devasari N4, Singh C4, Suresh S5, Jain S6. Carbohydr Polym. 2016 Feb 10;137:339-49. doi: 10.1016/j.carbpol.2015.10.080. Epub 2015 Oct 28.
The present study was envisaged to evaluate the effect of erlotinib β-cyclodextrin nanosponge (ERL-NS) on the solubility, dissolution, in vitro cytotoxicity and oral bioavailability of erlotinib (ERL). Preliminary studies were conducted to select the optimized stoichiometry concentration of ERL and NS. The drug nanosponge complex comprising of 1:4 proportions of ERL and NS was prepared by freeze drying. ERL-NS formed nanoparticles of 372 ± 31 nm size with narrow size distribution (0.21 ± 0.07 PDI) and high zeta potential (-32.07 ± 4.58 mV). The complexation phenomenon was confirmed by DSC, SEM, PXRD, FTIR, and TEM studies. In vitro dissolution studies revealed an increased dissolution rate (2-folds) with an enhanced dissolution efficiency of the nanosponge complex in comparison to pure drug. In vitro cytotoxicity study and apoptosis assay in pancreatic cell lines (MIA PaCa-2 and PANC-1) indicates the increased toxicity of ERL-NS. Both, quantitative and qualitative cell uptake studies unveiled the higher uptake efficiency of ERL-NS than free drug.
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Bio Calculators
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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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g/mol
Tip: Chemical formula is case sensitive. C22H30N4O √ c22h30n40 ╳