| Place of Origin: | CHINA |
|---|---|
| Brand Name: | TINGYI |
| Certification: | GMP , ISO 9001:2008 |
| Model Number: | 183319-69-9 |
| Minimum Order Quantity: | 10g |
| Price: | Negotiable ( Discounts For Big Order ) |
| Packaging Details: | Stealth And Discreet Packaging |
| Delivery Time: | Within 7 Working Days |
| Payment Terms: | Bank Transfer - Bitcoin - Western Union - MoneyGram |
| Product Name: | Erlotinib Hydrochloride | Other Name: | Erlotinib HCL |
|---|---|---|---|
| CAS: | 183319-69-9 | Appearance: | White Powder |
| Usage: | Small Molecule Tyrosine Kinase Inhibitor | Shipping Method: | EMS, HKEMS, FEDEX, DHL, UPS, Aramex, ETC |
| Grade Standard: | Medicine Grade | Purity: | 99% |
| Shelf Life: | 2 Years | ||
| High Light: | pharmaceutical active ingredients,pharmaceutical anabolic steroids |
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Erlotinib HCL
| Product Name: | Erlotinib hydrochloride |
| Synonyms: | Erlotinib HCl (OSI-744);Erlotinib hydrochloride, 98.5%;Tarceva, CP-358774;Erlotinib Hydrochloride WS;NSC 718781) HCl;Erlotinib hydrochloride N-(3-Ethynylphenyl)[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]amine hydrochloride;Erlotinib HCl, >=99%;CP-358774-01 |
| CAS: | 183319-69-9 |
| MF: | C22H24ClN3O4 |
| MW: | 429.9 |
| EINECS: | 620-491-0 |
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| Erlotinib hydrochloride Chemical Properties |
| Melting point | 223-225°C |
| storage temp. | -20°C Freezer |
| pka | pKa (25°): 5.42 |
| Erlotinib hydrochloride Usage And Synthesis |
| Indications and Usage | Erlotinib hydrochlorate is a small molecule tyrosine kinase inhibitor which acts reversibly on epidermal growth factor receptors, a hydrochloride of erlotinib, a molecular-targeted drug. The US Food and Drug Administration (FDA) has approved erlotinib (Tarceva) combined with gemcitabine as a first-line treatment for locally advanced and metastatic pancreatic cancer. It is mainly used as a second- or third-line treatment for locally advanced or metstatic non-small cell lung cancer (NSCLC) and as a treatment for pancreatic cancer. It is used as a tyrosine inhibitor for NSCLC treatment. |
| Mechanisms of Action | The small molecular compound erlotinib is a tyrosine kinase receptor inhibitor which inhibits the proliferation of tumor cells by inhibiting phosphorylation, binding to the intracellular catalytic domain of tyrosine kinase in competition with ATP, thus blocking downstream signal transduction and inhibiting activity of tumor cell ligand dependent HER-1/EGFR. |
| Clinical Research | Phase I clinical trials showed that the main toxicities and side effects of erlotinib were dose-dependent rashes and diarrhea. Other rare side effects included headaches, nausea, and vomiting. Phase II trials used erlotinib as a second-line anticancer drug, with efficacy matching second-line chemotherapy drug docetaxel. Phase III randomized control trials (BR21) mainly focused on NSCLC patients (locally advanced and distant metastasis) after the failure of first- or second-line chemotherapy. The treatment group, with 488 cases in total, took 150mg of erlotinib daily. The control group (243 cases) took a placebo. The study showed: Median survival rate: 6.7 months for the treatment group, 4.7 months for the control (P<0.001, hazard ratio HR=0.73) 1 year survival rate: 31.2% for the treatment group, 21.5% for the control Median time of no progression: 9.9 weeks for the treatment group, 7.9 weeks for the control Meanwhile, symptomatic improvement in the treatment group was more pronounced. Based on the results of the BR21 study, several further phase III clinical trials were conducted. The TRIBUTE trial combined erlotinib with chemotherapy. The treatment group used chemotherapy (carboplatin + paclitaxel) + erlotinib, while the control used the same chemotherapy alone, with a total of 1,059 late-stage NSCLC patients. The effectiveness of the treatment group was 21.5%, and the control group 19.3%; median survival times were 10.8 and 10.6 months, respectively, and the times of tumor progression (TTP) were 5.1 and 5.0 months. Meanwhile, TALENT trials, with 1,172 NSCLC patients, also investigated the effects of adding erlotinib to chemotherapy (gemcitabine + cisplatin), and also failed to show that erlotinib significantly increased its effects. |
| Chemical Properties | Off-White Solid |
| Uses | Selective epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor. Antineoplastic |
| Uses | Erlotinib HCl is an HER1/EGFR inhibitor with IC50 of 2 nM. |
| Uses | Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Phase 3. |
| Definition | ChEBI: A quinazoline hydrochloride compound having a (3-ethynylphenyl)amino group at the 4-position and two 2-methoxyethoxy groups at the 6- and 7-positions. |
| Brand name | Tarceva (OSI). |
| General Description | Erlotinib is available as 25-, 100-, and 150-mg tablets fororal administration and is used after failure of first-linetherapy in metastatic NSCLC and as first-line therapy incombination with gemcitabine in the treatment of metastaticpancreatic cancer, and in treating malignant gliomas.The structural similarity to gefitnib imparts similar pharmacokineticbehavior with bioavailability of 60% and proteinbinding of 93%. The agent is extensively metabolizedprimarily by CYP3A4. Three major metabolic pathwayshave been identified, involving oxidative-O-demethylationof the side chains followed by further oxidation to give thecarboxlic acids, oxidation of the acetylene functionalityto give a carboxylic acid, and aromatic hydroxylation ofthe phenyl ring para to the electron-donating nitrogen. Themetabolites are primarily eliminated in the feces, and theterminal half-life is 36 hours.The major toxicities seenwith the agent are dose-limiting skin rash and diarrhea.Other common adverse effects include shortness of breath,fatigue, and nausea. |
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