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  • 产品编号: 406106
  • 美  元  价: $90.00
  • 市  场  价: ¥1800.00
  • 品       牌:
  • 产       地: 美国(厂家直采)
  • 公       司: MedKoo Biosciences, Inc
  • 产品分类:
  • 公司分类: Angiogenesis
  • MedKoo/CL-387785newfeatured/10mg/406106


WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#:406106


Description: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.

Price and Availability

SizePriceShipping out timeQuantity
10mgUSD 90Same day
25mgUSD 150Same day
50mgUSD 250Same day
100mgUSD 450Same day
200mgUSD 750Same day
500mgUSD 1250Same day
1gUSD 1950Same day
2gUSD 3450Same day
5gUSD 56502 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-01-23.Prices are subject to change without notice.

CL-387785, purity > 98%, is in stock. The same day shipping out after order is received.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 406106Name: CL-387785CAS#: 194423-06-8Chemical Formula: C18H13BrN4OExact Mass: 380.02727Molecular Weight: 381.23Elemental 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.

IUPAC/Chemical Name:N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide


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)


Technical Data

Solid powder

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:
View CoA: current batch, Lot#TZC60217

QC Data:
View QC data: current batch, Lot#TZC60217

Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)

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).

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:

Additional Information


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

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

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

6: Chung JH, Rho JK, Xu X, Lee JS, Yoon HI, Lee CT, Choi YJ, Kim HR, KimCH, Lee JC. Clinical and molecular evidences of epithelial tomesenchymal 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 Dec17. PubMed PMID: 21168239.

7: Eisinger DA, Ammer H. Epidermal growth factor treatment switches δ-opioidreceptor-stimulated extracellular signal-regulated kinases 1 and 2signaling from an epidermal growth factor to an insulin-like growthfactor-1 receptor-dependent mechanism. Mol Pharmacol. 2011Feb;79(2):326-35. doi: 10.1124/mol.110.064956. Epub 2010 Nov 15. PubMedPMID: 21078885.

8: Yu Z, Boggon TJ, Kobayashi S, Jin C, Ma PC, Dowlati A, Kern JA, TenenDG, Halmos B. Resistance to an irreversible epidermal growth factorreceptor (EGFR) inhibitor in EGFR-mutant lung cancer reveals noveltreatment strategies. Cancer Res. 2007 Nov 1;67(21):10417-27. PubMedPMID: 17974985.

9: Kobayashi S, Shimamura T, Monti S, Steidl U, Hetherington CJ, LowellAM, Golub T, Meyerson M, Tenen DG, Shapiro GI, Halmos B. Transcriptionalprofiling identifies cyclin D1 as a critical downstream effector ofmutant epidermal growth factor receptor signaling. Cancer Res. 2006 Dec1;66(23):11389-98. PubMed PMID: 17145885.

10: Engelman JA, Mukohara T, Zejnullahu K, Lifshits E, Borrás AM, GaleCM, Naumov GN, Yeap BY, Jarrell E, Sun J, Tracy S, Zhao X, Heymach JV,Johnson BE, Cantley LC, Jänne PA. Allelic dilution obscures detection ofa biologically significant resistance mutation in EGFR-amplified lungcancer. J Clin Invest. 2006 Oct;116(10):2695-706. Epub 2006 Aug 10.PubMed PMID: 16906227; PubMed Central PMCID: PMC1570180.

11: Greulich H, Chen TH, Feng W, Jänne PA, Alvarez JV, Zappaterra M,Bulmer SE, Frank DA, Hahn WC, Sellers WR, Meyerson M. Oncogenictransformation by inhibitor-sensitive and -resistant EGFR mutants. PLoSMed. 2005 Nov;2(11):e313. Epub 2005 Oct 4. PubMed PMID: 16187797; PubMedCentral PMCID: PMC1240052.

12: Kobayashi S, Ji H, Yuza Y, Meyerson M, Wong KK, Tenen DG, Halmos B.An alternative inhibitor overcomes resistance caused by a mutation ofthe epidermal growth factor receptor. Cancer Res. 2005 Aug15;65(16):7096-101. PubMed PMID: 16103058.

13: Desai AA, Ratain MJ. EGFR pharmacogenomics: the story continues tomutate and evolve. Am J Pharmacogenomics. 2005;5(2):137-9. PubMed PMID:15813677.

14: Sweeney WE, Chen Y, Nakanishi K, Frost P, Avner ED. Treatment ofpolycystic kidney disease with a novel tyrosine kinase inhibitor. KidneyInt. 2000 Jan;57(1):33-40. PubMed PMID: 10620185.

15: Sweeney WE, Futey L, Frost P, Avner ED. In vitro modulation of cystformation by a novel tyrosine kinase inhibitor. Kidney Int. 1999Aug;56(2):406-13. PubMed PMID: 10432378.

16: Discafani CM, Carroll ML, Floyd MB Jr, Hollander IJ, Husain Z,Johnson BD, Kitchen D, May MK, Malo MS, Minnick AA Jr, Nilakantan R,Shen R, Wang YF, Wissner A, Greenberger LM. Irreversible inhibition ofepidermal growth factor receptor tyrosine kinase with in vivo activityby N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide(CL-387,785). Biochem Pharmacol. 1999 Apr 15;57(8):917-25. PubMed PMID:10086326.




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MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(Research Triangle Park, 简称 RTP ),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
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