Erlotinib hydrochloride

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MedKoo CAT#: 100300

CAS#: 183319-69-9 (HCl)

Description: Erlotinib hydrochloride is the hydrochloride salt of a quinazoline derivative with antineoplastic properties. Competing with adenosine triphosphate, erlotinib reversibly binds to the intracellular catalytic domain of epidermal growth factor receptor (EGFR) tyrosine kinase, thereby reversibly inhibiting EGFR phosphorylation and blocking the signal transduction events and tumorigenic effects associated with EGFR activation.

Chemical Structure

Erlotinib hydrochloride
CAS# 183319-69-9 (HCl)

Theoretical Analysis

MedKoo Cat#: 100300
Name: Erlotinib hydrochloride
CAS#: 183319-69-9 (HCl)
Chemical Formula: C22H24ClN3O4
Exact Mass:
Molecular Weight: 429.9
Elemental Analysis: C, 61.47; H, 5.63; Cl, 8.25; N, 9.77; O, 14.89

Price and Availability

Size Price Availability Quantity
5.0g USD 150.0 Same day
10.0g USD 250.0 Same day
20.0g USD 450.0 Same day
50.0g USD 650.0 Same day
100.0g USD 1050.0 Same day
200.0g USD 1750.0 Same day
500.0g USD 2950.0 Same day
1.0kg USD 3950.0 2 weeks
2.0kg USD 5950.0 2 weeks
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Related CAS #: 183319-69-9 (HCl)   183321-74-6 (free base)   248594-19-6 (mesylaye)    

Synonym: CP-358,774; CP-358774; CP358774; OSI-774; OSI 774; OSI774; Erlotinib hydrochloride; US brand name: Tarceva.

IUPAC/Chemical Name: N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine Monohydrochloride.


InChi Code: 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


Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO at 18 mg/mL with warming; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 5-20 µM.

Shelf Life: >10 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 429.9 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Gao JW, Zhan P, Qiu XY, Jin JJ, Lv TF, Song Y. Erlotinib-based doublet targeted therapy versus erlotinib alone in previously treated advanced non-small-cell lung cancer: a meta-analysis from 24 randomized controlled trials. Oncotarget. 2017 May 31;8(42):73258-73270. doi: 10.18632/oncotarget.18319. eCollection 2017 Sep 22. Review. PubMed PMID: 29069867; PubMed Central PMCID: PMC5641210.

2: Lee CK, Davies L, Wu YL, Mitsudomi T, Inoue A, Rosell R, Zhou C, Nakagawa K, Thongprasert S, Fukuoka M, Lord S, Marschner I, Tu YK, Gralla RJ, Gebski V, Mok T, Yang JC. Gefitinib or Erlotinib vs Chemotherapy for EGFR Mutation-Positive Lung Cancer: Individual Patient Data Meta-Analysis of Overall Survival. J Natl Cancer Inst. 2017 Jun 1;109(6). doi: 10.1093/jnci/djw279. Review. PubMed PMID: 28376144.

3: Yang Z, Hackshaw A, Feng Q, Fu X, Zhang Y, Mao C, Tang J. Comparison of gefitinib, erlotinib and afatinib in non-small cell lung cancer: A meta-analysis. Int J Cancer. 2017 Jun 15;140(12):2805-2819. doi: 10.1002/ijc.30691. Epub 2017 Mar 27. Review. PubMed PMID: 28295308.

4: How J, Mann J, Laczniak AN, Baggstrom MQ. Pulsatile Erlotinib in EGFR-Positive Non-Small-Cell Lung Cancer Patients With Leptomeningeal and Brain Metastases: Review of the Literature. Clin Lung Cancer. 2017 Jul;18(4):354-363. doi: 10.1016/j.cllc.2017.01.013. Epub 2017 Feb 9. Review. PubMed PMID: 28245967.

5: Rossi A, La Salvia A, Di Maio M. Chemotherapy and intercalated gefitinib or erlotinib in the treatment of advanced non-small-cell lung cancer. Expert Rev Respir Med. 2017 Mar;11(3):171-180. doi: 10.1080/17476348.2017.1290526. Epub 2017 Feb 9. Review. PubMed PMID: 28152323.

6: Zhang J, Zong Y, Xu GZ, Xing K. Erlotinib for advanced hepatocellular carcinoma. A systematic review of phase II/III clinical trials. Saudi Med J. 2016 Nov;37(11):1184-1190. doi: 10.15537/smj.2016.11.16267. Review. PubMed PMID: 27761555; PubMed Central PMCID: PMC5303794.

7: Xu W, Gong Y, Kuang M, Wu P, Cao C, Chen J, Tang C. Survival Benefit and Safety of Bevacizumab in Combination with Erlotinib as Maintenance Therapy in Patients with Metastatic Colorectal Cancer: A Meta-Analysis. Clin Drug Investig. 2017 Feb;37(2):155-165. doi: 10.1007/s40261-016-0465-0. Review. PubMed PMID: 27665469.

8: Gass-Jégu F, Gschwend A, Gairard-Dory AC, Mennecier B, Tebacher-Alt M, Gourieux B, Quoix É. Gastrointestinal perforations in patients treated with erlotinib: A report of two cases with fatal outcome and literature review. Lung Cancer. 2016 Sep;99:76-8. doi: 10.1016/j.lungcan.2016.06.012. Epub 2016 Jun 14. Review. PubMed PMID: 27565918.

9: Zhang S, Mao XD, Wang HT, Cai F, Xu J. Efficacy and safety of bevacizumab plus erlotinib versus bevacizumab or erlotinib alone in the treatment of non-small-cell lung cancer: a systematic review and meta-analysis. BMJ Open. 2016 Jun 30;6(6):e011714. doi: 10.1136/bmjopen-2016-011714. Review. PubMed PMID: 27363819; PubMed Central PMCID: PMC4932259.

10: Wang Y, Hu GF, Zhang QQ, Tang N, Guo J, Liu LY, Han X, Wang X, Wang ZH. Efficacy and safety of gemcitabine plus erlotinib for locally advanced or metastatic pancreatic cancer: a systematic review and meta-analysis. Drug Des Devel Ther. 2016 Jun 13;10:1961-72. doi: 10.2147/DDDT.S105442. eCollection 2016. Review. PubMed PMID: 27358556; PubMed Central PMCID: PMC4912328.

11: Zheng MH, Sun HT, Xu JG, Yang G, Huo LM, Zhang P, Tian JH, Yang KH. Combining Whole-Brain Radiotherapy with Gefitinib/Erlotinib for Brain Metastases from Non-Small-Cell Lung Cancer: A Meta-Analysis. Biomed Res Int. 2016;2016:5807346. doi: 10.1155/2016/5807346. Epub 2016 Feb 24. Review. PubMed PMID: 27006948; PubMed Central PMCID: PMC4783530.

12: Brower JV, Robins HI. Erlotinib for the treatment of brain metastases in non-small cell lung cancer. Expert Opin Pharmacother. 2016;17(7):1013-21. doi: 10.1517/14656566.2016.1165206. Epub 2016 Mar 30. Review. PubMed PMID: 26967582.

13: Awad R, Nott L. Radiation recall pneumonitis induced by erlotinib after palliative thoracic radiotherapy for lung cancer: Case report and literature review. Asia Pac J Clin Oncol. 2016 Mar;12(1):91-5. doi: 10.1111/ajco.12447. Epub 2016 Feb 5. Review. PubMed PMID: 26846159.

14: Jensen LH. Clinical aspects and perspectives of erlotinib in the treatment of patients with biliary tract cancer. Expert Opin Investig Drugs. 2016;25(3):359-65. doi: 10.1517/13543784.2016.1142973. Epub 2016 Feb 6. Review. PubMed PMID: 26781267.

15: Ma H, Tian X, Zeng XT, Zhang Y, Wang Y, Wang F, Zhou JG. The Efficacy of Erlotinib Versus Conventional Chemotherapy for Advanced Nonsmall-Cell Lung Cancer: A PRISMA-Compliant Systematic Review With Meta-Regression and Meta-Analysis. Medicine (Baltimore). 2016 Jan;95(2):e2495. doi: 10.1097/MD.0000000000002495. Review. PubMed PMID: 26765461; PubMed Central PMCID: PMC4718287.

16: Zhou JG, Tian X, Cheng L, Zhou Q, Liu Y, Zhang Y, Bai YJ, Ma H. The Risk of Neutropenia and Leukopenia in Advanced Non-Small Cell Lung Cancer Patients Treated With Erlotinib: A Prisma-Compliant Systematic Review and Meta-Analysis. Medicine (Baltimore). 2015 Oct;94(40):e1719. doi: 10.1097/MD.0000000000001719. Review. Erratum in: Medicine (Baltimore). 2015 Dec;94(51):e003b. PubMed PMID: 26448029; PubMed Central PMCID: PMC4616758.

17: Xu JL, Jin B, Ren ZH, Lou YQ, Zhou ZR, Yang QZ, Han BH. Chemotherapy plus Erlotinib versus Chemotherapy Alone for Treating Advanced Non-Small Cell Lung Cancer: A Meta-Analysis. PLoS One. 2015 Jul 6;10(7):e0131278. doi: 10.1371/journal.pone.0131278. eCollection 2015. Review. PubMed PMID: 26147288; PubMed Central PMCID: PMC4493135.

18: Greenhalgh J, Bagust A, Boland A, Dwan K, Beale S, Hockenhull J, Proudlove C, Dundar Y, Richardson M, Dickson R, Mullard A, Marshall E. Erlotinib and gefitinib for treating non-small cell lung cancer that has progressed following prior chemotherapy (review of NICE technology appraisals 162 and 175): a systematic review and economic evaluation. Health Technol Assess. 2015 Jun;19(47):1-134. doi: 10.3310/hta19470. Review. PubMed PMID: 26134145; PubMed Central PMCID: PMC4781386.

19: Ellis PM, Coakley N, Feld R, Kuruvilla S, Ung YC. Use of the epidermal growth factor receptor inhibitors gefitinib, erlotinib, afatinib, dacomitinib, and icotinib in the treatment of non-small-cell lung cancer: a systematic review. Curr Oncol. 2015 Jun;22(3):e183-215. doi: 10.3747/co.22.2566. Review. PubMed PMID: 26089730; PubMed Central PMCID: PMC4462541.

20: Landi L, Cappuzzo F. Experience with erlotinib in the treatment of non-small cell lung cancer. Ther Adv Respir Dis. 2015 Aug;9(4):146-63. doi: 10.1177/1753465815588053. Epub 2015 Jun 10. Review. PubMed PMID: 26063687.