Ko 143
461054-93-3
0.98%
2026-07-18
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
-
Product Description
-
Seller Information
-
Description
ProductName Ko 143 Cat No CEI-1388 Description Ko 143 is potent and selective inhibitor of breast cancer resistance protein multidrug transporter (BCRP) with an EC90 value of 26 nM. Product Overview Ko 143 is a potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor with IC50 value of 26 nM. BCRP is a member of ATP-binding cassette transport protein superfamily, which is a plasma membrane protein associated with multidrug resistance of cancer cells. It is found in the intestinal epithelium, liver canaliculi, the placental trophoblasts, mammary ducts and lobules, and endothelial cells of veins and capillaries. MDR is the principal reason for the failure of anticancer chemotherapy, where BCRP may act as a broad specificity drug efflux pump and confer multidrug resistance. When overexpressed, BCRP is able to confer the resistance of various cancer cell lines to drugs including topotecan, doxorubicin, daunorubicin and mitoxantrone. BCRP is the first potent and specific BCRP inhibitor applicable in vivo. When a library of potent compounds was screened in mouse T6400 and human T8 cancer cell line, Ko 143 was identified as the inhibitor with the high inhibitory activity and low cytotoxicity. Additionally, Ko 143 was observed to have 200-fold selectivity over P-glycoprotein and multidrug resistance protein-1.The effect of Ko 143 in reversing Bcrp-1/BCRP-mediated drug resistance was also observed in mouse T6400 and human T8 cell line respectively. At EC90 concentration of Ko 143, it reversed the Bcrp-1/BCRP-mediated drug resistance in the drug selected T6400 and T8 cell line, resulting in 10-fold sensitization to topotecan and mitoxantrone. In mouse model, oral administration of Ko 143 50 mg/day or higher showed no evidence of acute of delayed cellular toxicity. In Mdr1a/1b-/-mice, oral administration of Ko 143 of 10 mg/kg resulted in increasing plasma topotecan level by 4-6 folds at 30 min and 60 min after oral administration of the drug. It suggested Ko 143 suppressed the multidrug resistance conferred by BCRP. CAS No 461054-93-3 Molecular Weight 469.59 Purity 0.98 Storage Store at -20°C Synonyms Ko-143; Ko143 Targets BCRP IC50 26 nM (EC90) Molecular Formula C26H35N3O5 Chemical Name tert-butyl 3-((3R,6S,12aR)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino[1,2:1,6]pyrido[3,4-b]indol-3-yl)propanoate Solubility Soluble in DMSO > 10 mM Shipping Conditions Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request category Specialty Chemicals(c26) cas_num 461054-93-3 Basic Info-
Product Name:
(3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino[1',2':1,6]pyrido[3,4-b]indole-3-propanoicacid1,1-dimethylethylester
Other Name:Pyrazino[1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid, 1,2,3,4,6,7,12,12a-octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxo-, 1,1-dimethylethyl ester, (3S,6S,12aS)-(Ko143);Ko 143;(3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino[1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester;12a-octahydro-9-Methoxy-6-(2-Methylpropyl)-1;12aS)-;4-b]indole-3-propanoicacid;4-dioxo-;6]pyrido[3
CAS No.:461054-93-3
Molecular Formula:C26H35N3O5
InChIKeys:NXNRAECHCJZNRF-JBACZVJFSA-N
Molecular Weight:469.57
Exact Mass:469.25767123
DSSTox ID:DTXSID30438079
Categories:
Characteristics-
PSA:
100.73000
XLogP3:3.90400
Density:1.24
Melting Point:147 ºC
Boiling Point:689.8±55.0 °C(Predicted)
Flash Point:371ºC
Refractive Index:1.597
PKA:13.31±0.60
-
-
Seller Information
-
Business Type:
Manufactory
-
Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
-
Location:
Shirley, New York 11967, USA
-
Payment Terms:
TT against copy of documents,D/P
-
Average lead Time:
15
-
Total Annual Revenue:
$1 million-$2.5 million
-
Year of Establishment:
2004
-
-
Country Product Purchase Quantity Date Posted Post an enquiry for this product