CL-387785 (Standard)
CL-387785 (EKI-785; WAY-EKI 785) (Standard) is the analytical standard of CL-387785 (HY-10325). This product is intended for research and analytical applications. CL-387785 is an orally active EGFR inhibitor with an IC50 of 370 pM. CL-387785 inhibits EGF-stimulated EGFR autophosphorylation with an IC50 of approximately 5 nM. CL-387,785 exerts selective inhibition on cell lines overexpressing EGFR or c-erbB-2, whereas it shows weak inhibitory effects on cell lines with low expression of these two receptors. CL-387785 effectively induces cell cycle arrest and apoptosis. CL-387785 can be used for the research of non-small cell lung cancer and autosomal recessive polycystic kidney disease.
For research use only. We do not sell to patients.
- CAS No.: 194423-06-8
- Formula: C18H13BrN4O
- Molecular Weight:381.23
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Product Information
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Chemical Information
- Purity & Documentation
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Help & FAQs
Product Information
The compound is the grade of analytical standard, which is the reference standard supplied assay. It is commonly used in qualitative, quantitative and methodological research experiments in HPLC, GC and MS.
Chemical Information
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CAS No. 194423-06-8
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Molecular Weight 381.23
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Formula C18H13BrN4O
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SMILES
O=C(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)C#CC
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Synonyms
EKI-785 (Standard); WAY-EKI 785 (Standard)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Discafani CM, et al. Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (CL-387,785). Biochem Pharmacol. 1999 Apr 15;57(8):917-25. [Content Brief]
[2]. Sweeney WE, et al. Treatment of polycystic kidney disease with a novel tyrosine kinase inhibitor. Kidney Int. 2000 Jan;57(1):33-40. [Content Brief]
[3]. Greulich H, et al. Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants. PLoS Med. 2005 Nov;2(11):e313. [Content Brief]
[4]. Kobayashi S, et al. An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor. Cancer Res. 2005 Aug 15;65(16):7096-101. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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