Icotinib
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MedKoo CAT#: 413263

CAS#: 610798-31-7

Description: Icotinib has antineoplastic activity.


Chemical Structure

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Icotinib
CAS# 610798-31-7

Theoretical Analysis

MedKoo Cat#: 413263
Name: Icotinib
CAS#: 610798-31-7
Chemical Formula: C22H21N3O4
Exact Mass: 391.1532
Molecular Weight: 391.43
Elemental Analysis: C, 67.51; H, 5.41; N, 10.74; O, 16.35

Price and Availability

Size Price Availability Quantity
1.0mg USD 205.0 2 Weeks
5.0mg USD 403.0 2 Weeks
10.0mg USD 650.0 2 Weeks
25.0mg USD 1088.0 2 Weeks
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Synonym: Icotinib; Conmana; BPI2009; BPI 2009; BPI-2009

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

InChi Key: QQLKULDARVNMAL-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H21N3O4/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)

SMILES Code: C#CC1=CC(NC2=C3C=C(OCCOCCOCCO4)C4=CC3=NC=N2)=CC=C1

Appearance: 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

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 391.43 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: 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. PMID: 23948351.

2: Shi YK, Wang L, Han BH, Li W, Yu P, Liu YP, Ding CM, Song X, Ma ZY, Ren XL, Feng JF, Zhang HL, Chen GY, Han XH, Wu N, Yao C, Song Y, Zhang SC, Song W, Liu XQ, Zhao SJ, Lin YC, Ye XQ, Li K, Shu YQ, Ding LM, Tan FL, Sun Y. First-line icotinib versus cisplatin/pemetrexed plus pemetrexed maintenance therapy for patients with advanced EGFR mutation-positive lung adenocarcinoma (CONVINCE): a phase 3, open-label, randomized study. Ann Oncol. 2017 Oct 1;28(10):2443-2450. doi: 10.1093/annonc/mdx359. PMID: 28945850.

3: Yang JJ, Zhou C, Huang Y, Feng J, Lu S, Song Y, Huang C, Wu G, Zhang L, Cheng Y, Hu C, Chen G, Zhang L, Liu X, Yan HH, Tan FL, Zhong W, Wu YL. Icotinib versus whole-brain irradiation in patients with EGFR-mutant non-small-cell lung cancer and multiple brain metastases (BRAIN): a multicentre, phase 3, open-label, parallel, randomised controlled trial. Lancet Respir Med. 2017 Sep;5(9):707-716. doi: 10.1016/S2213-2600(17)30262-X. Epub 2017 Jul 19. PMID: 28734822.

4: Zhao Q, Cheng J, Chen P, Sun J, Guan S. Icotinib: efficacy in different solid tumors and gene mutations. Anticancer Drugs. 2020 Mar;31(3):205-210. doi: 10.1097/CAD.0000000000000861. PMID: 31934888.

5: Li X, Zhang L, Jiang D, Wang Y, Zang A, Ding C, Zhao M, Su W, Zhang Y, Zhong D, Wu J, Zhang C, An G, Hu X, Cheng G, Wang H, Li Y, He X, Liu J, Liang L, Ding L, Mao L, Zhang S. Routine-Dose and High-Dose Icotinib in Patients with Advanced Non-Small Cell Lung Cancer Harboring EGFR Exon 21-L858R Mutation: the Randomized, Phase II, INCREASE Trial. Clin Cancer Res. 2020 Jul 1;26(13):3162-3171. doi: 10.1158/1078-0432.CCR-19-3064. Epub 2020 Feb 14. PMID: 32060099.

6: Lei L, Wang WX, Zhu YC, Li JL, Fang Y, Wang H, Zhuang W, Zhang YB, Wang LP, Fang MY, Xu CW, Wang XJ, Lv TF, Song Y. Potential mechanism of primary resistance to icotinib in patients with advanced non-small cell lung cancer harboring uncommon mutant epidermal growth factor receptor: A multi-center study. Cancer Sci. 2020 Feb;111(2):679-686. doi: 10.1111/cas.14277. Epub 2020 Jan 16. PMID: 31828849; PMCID: PMC7004544.

7: Zhou X, Hua D, Gao C, Zhang Y, Qiu L, Wang L. Icotinib and pemetrexed in treatment of lung adenocarcinoma and the effects on prognostic survival rate of patients. Oncol Lett. 2019 Oct;18(4):4153-4159. doi: 10.3892/ol.2019.10763. Epub 2019 Aug 16. PMID: 31516614; PMCID: PMC6732991.

8: Wang GH, Hu ZY. Icotinib inhibits proliferation and epithelial-mesenchymal transition of non-small cell lung cancer A549 cells. Math Biosci Eng. 2019 Aug 21;16(6):7707-7718. doi: 10.3934/mbe.2019386. PMID: 31698635.

9: Peng LY, Yu M, Yang MX, Liu P, Zhou H, Huang W, Kong H, Xie WP. Icotinib Attenuates Monocrotaline-Induced Pulmonary Hypertension by Preventing Pulmonary Arterial Smooth Muscle Cell Dysfunction. Am J Hypertens. 2020 Aug 4;33(8):775-783. doi: 10.1093/ajh/hpaa066. PMID: 32301965.

10: 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. PMID: 24588695.