| Identification | Back Directory | [Name]
Icotinib | [CAS]
610798-31-7 | [Synonyms]
ConMana
BP-1096
BPI-2009
Lcotinib
Icotinib
BPI-2009H
Icotinib int. N-1
N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin
N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine
[1,4,7,10]Tetraoxacyclododecino[2,3-g]quinazolin-4-amine, N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro- | [EINECS(EC#)]
1592732-453-0 | [Molecular Formula]
C22H21N3O4 | [MDL Number]
MFCD22124501 | [MOL File]
610798-31-7.mol | [Molecular Weight]
391.43 |
| Chemical Properties | Back Directory | [Boiling point ]
581℃ | [density ]
1.31 | [Fp ]
305℃ | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥129.6 mg/mL in DMSO; ≥14.13 mg/mL in EtOH with ultrasonic | [form ]
Powder | [pka]
5.32±0.20(Predicted) | [color ]
White to off-white | [InChIKey]
QQLKULDARVNMAL-UHFFFAOYSA-N | [SMILES]
N(c4cc(ccc4)C#C)c1ncnc2c1cc3c(c2)OCCOCCOCCO3 |
| Questions and Answers (Q&A) | Back Directory | [Description]
Icotinib is also known as ConMana. It is a highly selective, first-generation inhibitor of epidermal growth factor receptor tyrosine kinase (EGFR-TKI), whose mutation and overexpression is involved in many kinds of cancer. Icotinib is a quinazoline derivative that binds reversibly to the ATP binding site of the EGFR protein, being capable of blocking the signal transduction cascade. It is currently under investigation for its treatment efficacy on the EGFR+ Non-small cell lung cancer.
| [References]
Tan, F., et al. "Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. " Lung Cancer76.2(2012):177-82.
Shi, Y., et al. "Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial." Lancet Oncology 14.10(2013):953-61.
Sun, Y., Y. Shi, and L. Zhang. "A randomized, double-blind phase III study of icotinib versus gefitinib in patients with advanced non-small cell lung cancer (NSCLC) previously treated with chemotherapy (ICOGEN)."Journal of Thoracic Oncology 29.15(2011):-.
https://en.wikipedia.org/wiki/Icotinib
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| Questions And Answer | Back Directory | [Uses]
Icotinib is a highly selective, 1st generation EGFR-TKI (epidermal growth factor receptor tyrosine kinase) inhibitor. The mutations of EGFR is associated with many kinds of cancers. Currently, Icotinib is under investigation for its treatment efficacy on some cancer such as non-small cell lung cancer. Icotinib take effects through binding reversibly to the ATP binding site of the EGFR protein, further preventing completion of the signal transduction cascade.
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| Hazard Information | Back Directory | [Indications]
Icotinib (Conmana?, BetaPharma), an EGFR inhibitor, was approved by the China State FDA in 2011 for the treatment of NSCLC. Icotinib resembles erlotinib in possessing the N-(3-ethylnylphenyl) quinazolin-4-amine core scaffold of erlotinib that binds to the EGFR ATP pocket. An adjacent hydrophobic group was also retained while the solvent exposed two 2-methoxyethyoxysubstituents at the 6- and 7-positions of the quinazoline core were cyclized to afford the tetraoxacyclododecene moiety of icotinib. Efficacy and safety of icotinib as first-line therapy in patients has been evaluated for advanced NSCLC in recent clinical studies. | [General Description]
Class: receptor tyrosine kinase
Treatment: NSCLC
Oral bioavailability = 52%
Elimination half-life = 5.5 h
| [in vivo]
Icotinib exhibits potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug is well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. Icotinib inhibits tumor growth at a rate of 25.2%, 45.6% and 51.5% in the A431 cell line groups; 3.4%, 25.9% and 31.0% in the A549 cell line groups; 49.4%, 52.6% and 67.4% in the H460 cell line groups, and 30.3%, 36.4% and 46.5% in the HCT8 cell line groups, at 30, 60 and 120 mg/kg/dose, respectively[1]. | [IC 50]
EGFR: 5 nM (IC50); EGFRL858R; EGFRL858R/T790M; EGFRT790M; EGFRL861Q |
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| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
Struchem Co., Ltd.
|
| Telephone: |
0512-63009836 18994340901 |
| Website: |
http://www.beidapharma.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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