CL-387,785

Min.Order / FOB Price:Get Latest Price

100 Gram	FOB Price: USD 1.0000

100 Gram

FOB Price: USD 1.0000

Min.Order :100 Gram
Purity: 98%
Payment Terms : L/C

Keywords

CL-387,785 2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]-;CL-387785 (EKI-785);N-(4-(3-bromophenylamino)quinazolin-6-yl)but-2-ynamide;N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]-2-ButynaMide CL-387785 194423-06-8

Quick Details

Appearance:White crystal
Application:CAS：194423-06-8； Small molecule inhibitors
PackAge:100g,500g,1kg,25kg/drum
ProductionCapacity:1000|Gram|Month
Storage:Dry seal
Transportation:shipping

Superiority:

We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.

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Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.

Details:

CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level.
IC50 value: 370+/-120 pM
Target: EGFR
in vitro: CL-387785 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 [1]. Whereas transformation by most EGFR mutants confers on cells sensitivity to erlotinib and gefitinib, transformation by an exon 20 insertion makes cells resistant to these inhibitors but more sensitive to the irreversible inhibitor CL-387,785 [3]. CL-387,785 is able to overcome resistance caused by the T790M mutation on a functional level, correlating with effective inhibition of downstream signaling pathways [4].
in vivo: CL-387785 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) [1]. Treatment of BPK mice with EKI-785 resulted in a marked reduction of collecting tubule (CT) cystic lesions, improved renal function, decreased biliary epithelial abnormalities, and an increased life span. Cystic animals treated with EKI-785 to postnatal day 48 (P-48) were alive and well with normal renal function, a reduced CT cystic index of 2.0 (P < 0.02), a threefold increased in maximum urinary concentrating ability (P < 0.01), and a significant decrease in biliary epithelial proliferation/fibrosis (P < 0.01) [2].