Icotinib HCl

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MedKoo CAT#: 205847

CAS#: 1204313-51-8 (HCl)

Description: Icotinib, also known as BPI-2009, is an orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Icotinib selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. This may lead to an inhibition of EGFR-mediated signal transduction and may inhibit cancer cell proliferation. EGFR, a receptor tyrosine kinase, is upregulated in a variety of cancer cell types.

Chemical Structure

Icotinib HCl
CAS# 1204313-51-8 (HCl)

Theoretical Analysis

MedKoo Cat#: 205847
Name: Icotinib HCl
CAS#: 1204313-51-8 (HCl)
Chemical Formula: C22H22ClN3O4
Exact Mass:
Molecular Weight: 427.89
Elemental Analysis: C, 61.76; H, 5.18; Cl, 8.28; N, 9.82; O, 14.96

Price and Availability

Size Price Availability Quantity
10.0mg USD 90.0 Same day
25.0mg USD 150.0 Same day
50.0mg USD 250.0 Same day
100.0mg USD 450.0 Same day
200.0mg USD 750.0 Same day
500.0mg USD 1550.0 Same day
1.0g USD 2450.0 Same day
2.0g USD 3650.0 2 weeks
5.0g USD 5850.0 2 weeks
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Related CAS #: 1204313-51-8 (HCl)   610798-31-7 (free base)    

Synonym: BPI2009; BPI 2009; BPI-2009; Icotinib; Brand name: Conmana.

IUPAC/Chemical Name: N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride


InChi Code: InChI=1S/C22H21N3O4.ClH/c1-2-16-4-3-5-17(12-16)25-22-18-13-20-21(14-19(18)23-15-24-22)29-11-9-27-7-6-26-8-10-28-20;/h1,3-5,12-15H,6-11H2,(H,23,24,25);1H


Appearance: Light yellow 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, not in water

Shelf Life: >2 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 427.89 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: Chen X, Zhu Q, Liu Y, Liu P, Yin Y, Guo R, Lu K, Gu Y, Liu L, Wang J, Wang Z, Røe OD, Shu Y, Zhu L. Icotinib is an active treatment of non-small-cell lung cancer: a retrospective study. PLoS One. 2014 May 16;9(5):e95897. doi: 10.1371/journal.pone.0095897. eCollection 2014. PubMed PMID: 24836053; PubMed Central PMCID: PMC4023939.

2: Pan H, Liu R, Li S, Fang H, Wang Z, Huang S, Zhou J. Effects of Icotinib on Advanced Non-Small Cell Lung Cancer with Different EGFR Phenotypes. Cell Biochem Biophys. 2014 Apr 29. [Epub ahead of print] PubMed PMID: 24777808.

3: Guan YS, He Q, Li M. Icotinib: activity and clinical application in Chinese patients with lung cancer. Expert Opin Pharmacother. 2014 Apr;15(5):717-28. doi: 10.1517/14656566.2014.890183. Epub 2014 Mar 4. PubMed PMID: 24588695.

4: Liang W, Wu X, Fang W, Zhao Y, Yang Y, Hu Z, Xue C, Zhang J, Zhang J, Ma Y, Zhou T, Yan Y, Hou X, Qin T, Dinglin X, Tian Y, Huang P, Huang Y, Zhao H, Zhang L. Network meta-analysis of erlotinib, gefitinib, afatinib and icotinib in patients with advanced non-small-cell lung cancer harboring EGFR mutations. PLoS One. 2014 Feb 12;9(2):e85245. doi: 10.1371/journal.pone.0085245. eCollection 2014. PubMed PMID: 24533047; PubMed Central PMCID: PMC3922700.

5: Liu D, Jiang J, Zhang L, Tan F, Wang Y, Zhang D, Hu P. Clinical pharmacokinetics of Icotinib, an anti-cancer drug: evaluation of dose proportionality, food effect, and tolerability in healthy subjects. Cancer Chemother Pharmacol. 2014 Apr;73(4):721-7. doi: 10.1007/s00280-014-2398-8. Epub 2014 Feb 1. PubMed PMID: 24488324.

6: Shao L, Zhang B, He C, Lin B, Song Z, Lou G, Yu X, Zhang Y. Efficacy and safety of icotinib in Chinese patients with advanced non-small cell lung cancer after failure of chemotherapy. Chin Med J (Engl). 2014;127(2):266-71. PubMed PMID: 24438614.

7: Guan Y, Zhao H, Meng J, Yan X, Jiao S. Dramatic response to high-dose icotinib in a lung adenocarcinoma patient after erlotinib failure. Lung Cancer. 2014 Feb;83(2):305-7. doi: 10.1016/j.lungcan.2013.12.002. Epub 2013 Dec 12. PubMed PMID: 24370197.

8: Zhao Q, Wang Y, Tang Y, Peng L. Icotinib combined with rapamycin in a renal transplant recipient with epidermal growth factor receptor-mutated non-small cell lung cancer: A case report. Oncol Lett. 2014 Jan;7(1):171-176. Epub 2013 Nov 5. PubMed PMID: 24348843; PubMed Central PMCID: PMC3861587.

9: Sun X, Zheng Y. Retreatment with icotinib in a patient with metastatic lung adenocarcinoma. Tumori. 2013 May-Jun;99(3):e124-6. doi: 10.1700/1334.14820. PubMed PMID: 24158081.

10: Shi Y, Zhang L, Liu X, Zhou C, Zhang L, Zhang S, Wang D, Li Q, Qin S, Hu C, Zhang Y, Chen J, Cheng Y, Feng J, Zhang H, Song Y, Wu YL, Xu N, Zhou J, Luo R, Bai C, Jin Y, Liu W, Wei Z, Tan F, Wang Y, Ding L, Dai H, Jiao S, Wang J, Liang L, Zhang W, Sun Y. Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial. Lancet Oncol. 2013 Sep;14(10):953-61. doi: 10.1016/S1470-2045(13)70355-3. Epub 2013 Aug 13. PubMed PMID: 23948351.

11: Camidge DR. Icotinib: kick-starting the Chinese anticancer drug industry. Lancet Oncol. 2013 Sep;14(10):913-4. doi: 10.1016/S1470-2045(13)70385-1. Epub 2013 Aug 13. PubMed PMID: 23948350.

12: Yang X, Zhang H, Qin N, Li X, Nong J, Lv J, Wu Y, Zhang Q, Zhang S. [Clinical observation of icotinib hydrochloride in first-line therapy for pulmonary adenocarcinoma]. Zhongguo Fei Ai Za Zhi. 2013 Jul;16(7):364-8. doi: 10.3779/j.issn.1009-3419.2013.07.06. Chinese. PubMed PMID: 23866667.

13: Nong J, Qin N, Wang J, Yang X, Zhang H, Wu Y, Lv J, Zhang Q, Zhang S. [Clinical effects for patients with recurrent advanced non-small cell lung cancer treated with icotinib hydrochloride]. Zhongguo Fei Ai Za Zhi. 2013 May;16(5):240-5. doi: 10.3779/j.issn.1009-3419.2013.05.05. Chinese. PubMed PMID: 23676980.

14: Lv C, Ma Y, Feng Q, Fang F, Bai H, Zhao B, Yan S, Wu N, Zheng Q, Li S, Chen J, Wang J, Feng Y, Wang Y, Pei Y, Fang J, Yang Y. A pilot study: sequential gemcitabine/cisplatin and icotinib as induction therapy for stage IIB to IIIA non-small-cell lung adenocarcinoma. World J Surg Oncol. 2013 Apr 26;11:96. doi: 10.1186/1477-7819-11-96. PubMed PMID: 23621919; PubMed Central PMCID: PMC3643858.

15: Gao Z, Chen W, Zhang X, Cai P, Fang X, Xu Q, Sun Y, Gu Y. Icotinib, a potent and specific EGFR tyrosine kinase inhibitor, inhibits growth of squamous cell carcinoma cell line A431 through negatively regulating AKT signaling. Biomed Pharmacother. 2013 Jun;67(5):351-6. doi: 10.1016/j.biopha.2013.03.012. Epub 2013 Apr 2. PubMed PMID: 23602321.

16: Mu X, Zhang Y, Qu X, Hou K, Kang J, Hu X, Liu Y. Ubiquitin ligase Cbl-b is involved in icotinib (BPI-2009H)-induced apoptosis and G1 phase arrest of EGFR mutation-positive non-small-cell lung cancer. Biomed Res Int. 2013;2013:726375. doi: 10.1155/2013/726375. Epub 2013 Mar 19. PubMed PMID: 23586056; PubMed Central PMCID: PMC3615596.

17: Song Z, Yu X, Cai J, Shao L, Lin B, He C, Zhang B, Zhang Y. [Efficacy of icotinib for advanced non-small cell lung cancer patients with EGFR status identified]. Zhongguo Fei Ai Za Zhi. 2013 Mar;16(3):138-43. doi: 10.3779/j.issn.1009-3419.2013.03.04. Chinese. PubMed PMID: 23514942.

18: Gu A, Shi C, Xiong L, Chu T, Pei J, Han B. Efficacy and safety evaluation of icotinib in patients with advanced non-small cell lung cancer. Chin J Cancer Res. 2013 Feb;25(1):90-4. doi: 10.3978/j.issn.1000-9604.2012.12.07. PubMed PMID: 23372346; PubMed Central PMCID: PMC3555305.

19: Zhao Q, Wang YN, Wang B. Spared pre-irradiated area in pustular lesions induced by icotinib showing decreased expressions of CD1a+ langerhans cells and FGFR2. Jpn J Clin Oncol. 2013 Feb;43(2):200-4. doi: 10.1093/jjco/hys209. Epub 2012 Dec 21. PubMed PMID: 23264674.

20: Zheng Y, Fang W, Xu N. Hand-foot syndrome in a patient with metastatic lung adenocarcinoma induced by high-dose icotinib: A case report and review of the literature. Oncol Lett. 2012 Dec;4(6):1341-1343. Epub 2012 Sep 10. PubMed PMID: 23205134; PubMed Central PMCID: PMC3506748.

Additional Information

Icotinib was approved in China in 2011.