CL-387785


Catalog No. size PriceQuantity
M7079-2 2mg solid $120
M7079-10 10mg solid $476

Description

 

Cas:194423-06-8

Product Information

CL-387785, also known as EKI-785 , is a n irreversible inhibitor of EGF-receptor (EGFR) kinase activity in vivo (IC50 = 250-490 pM). CL-387785 covalently bound to EGF-R. It also specifically inhibited kinase activity of the protein (IC50 = 370+/-120 pM), blocked EGF-stimulated autophosphorylation of the receptor in cells (ic50 approximately 5 nM), inhibited cell proliferation (IC50 = 31-125 nM) primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2, and profoundly blocked the growth of a tumor that overexpresses EGF-R in nude mice (when given orally at 80 mg/kg/day for 10 days, daily). CL-387,785 is useful for studying the interaction of small molecules with EGF-R and may have clinical utility.

 

Chemical Formula: C18H13BrN4O

 

Exact Mass: 380.02727

 

Molecular Weight: 381.23

 

Elemental Analysis: C, 56.71; H, 3.44; Br, 20.96; N, 14.70; O, 4.20

 

Synonym: 

 

CL387785

CL 387785

CL-387785

EKI785

EK-I785

EK I785

 

Chemical Name:

N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide

 

InChi Key: 

BTYYWOYVBXILOJ-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C18H13BrN4O/c1-2-4-17(24)22-14-7-8-16-15(10-14)18(21-11-20-16)23-13-6-3-5-12(19)9-13/h3,5-11H,1H3,(H,22,24)(H,20,21,23)

 

Smiles Code:

CC#CC(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)=O

 

 

Technical Data:

 

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, 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

 

 

References

 

  1. Tomioka H, Mukohara T, Kataoka Y, Ekyalongo RC, Funakoshi Y, Imai Y, Kiyota N, Fujiwara Y, Minami H. Inhibition of the mTOR/S6K signal is necessary to enhance fluorouracil-induced apoptosis in gastric cancer cells with HER2 amplification. Int J Oncol. 2012 Aug;41(2):551-8. doi: 10.3892/ijo.2012.1485. Epub 2012 May 17. PubMed PMID: 22614071.

 

  1. Chiu HC, Chang TY, Huang CT, Chao YS, Hsu JT. EGFR and myosin II inhibitors cooperate to suppress EGFR-T790M-mutant NSCLC cells. Mol Oncol. 2012 Jun;6(3):299-310. doi: 10.1016/j.molonc.2012.02.001. Epub 2012 Feb 10. PubMed PMID: 22366308.

 

  1. Zannetti A, Iommelli F, Speranza A, Salvatore M, Del Vecchio S. 3'-deoxy-3'-18F-fluorothymidine PET/CT to guide therapy with epidermal growth factor receptor antagonists and Bcl-xL inhibitors in non-small cell lung cancer. J Nucl Med. 2012 Mar;53(3):443-50. doi: 10.2967/jnumed.111.096503. Epub 2012 Feb 13. PubMed PMID: 22331221.

 

  1. Kancha RK, von Bubnoff N, Bartosch N, Peschel C, Engh RA, Duyster J. Differential sensitivity of ERBB2 kinase domain mutations towards lapatinib. PLoS One. 2011;6(10):e26760. doi: 10.1371/journal.pone.0026760. Epub 2011 Oct 28. PubMed PMID: 22046346; PubMed Central PMCID: PMC3203921.

 

  1. Hama T, Yuza Y, Suda T, Saito Y, Norizoe C, Kato T, Moriyama H, Urashima M. Functional mutation analysis of EGFR family genes and corresponding lymph node metastases in head and neck squamous cell carcinoma. Clin Exp Metastasis. 2012 Jan;29(1):19-25. doi: 10.1007/s10585-011-9425-5. Epub 2011 Sep 28. PubMed PMID: 21953075.

 

  1. Chung JH, Rho JK, Xu X, Lee JS, Yoon HI, Lee CT, Choi YJ, Kim HR, Kim CH, Lee JC. Clinical and molecular evidences of epithelial to mesenchymal transition in acquired resistance to EGFR-TKIs. Lung Cancer. 2011 Aug;73(2):176-82. doi: 10.1016/j.lungcan.2010.11.011. Epub 2010 Dec 17. PubMed PMID: 21168239.

 

Products are for research use only. Not for human use.

 

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