A-443654
552325-16-3
0.98%
2026-06-26
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName A-443654 Cat No CEI-1194 Description A-443654 is a potent and selective inhibitor of Akt1 with Ki value of 160 pM. Product Overview A-443654 is a potent and selective inhibitor of Akt with Ki value of 160 pM. The Akt kinases play important roles in cellular signal transduction and take participate in the regulation of cell transformation and tumor progression. The activities of them are usually elevated in human malignancies. A-443654 is a pan inhibitor of Akt1, 2 and 3. It binds to the ATP-binding site of Akt and inhibits the kinase activity reversibly. A-443654 shows selectivity against Akt. The inhibition ability of it for Akt is much higher than that for other kinases. It is found that A-443654 can suppress the phosphorylation of the downstream proteins of Akt while increased the Ser473 and Thr308 phosphorylation of Akt. In murine FL5.12 cells stably transfected with human Akt1, 2 or 3, A-443654 inhibited the phosphorylation of GSK3 dose-dependently. A-443654 at a concentration of 0.6 μM inhibited Akt and induced G2/M accumulation in H1299 cells. In MiaPaCa-2 cells, treatment of A-443654 for 48 h resulted in a suppression of tumor proliferation with EC50 value of 100 nM. In chronic lymphocytic leukemia cells, A-443654 also inhibited the activity of Akt and induced apoptosis with EC50 value of 0.63 μM. Besides that, A-443654 was found to cause decreased phosphorylation of GSK3, FOXO3, TSC2 and mTOR in MiaPaCa-2 cells. It is also reported that A-443654 was effective in blocking the phosphorylation of 4EBP-1 and S6 protein in both T47D and LNCaP cells. A-443654 is not oral available. In mice model with human MiaPaCa-2 pancreatic cell xenograft, the administration of A-443654 at a dose of 7.5mg/kg/d significantly inhibited tumor growth. A-443654 also inhibited tumor growth in 3T3 murine fibroblast model expressing active Akt. When using the combination of A-443654 and rapamycin in mice model with MiaPaCa-2 pancreatic cancer xenograft, the administration showed more efficacy than each monotherapy CAS No 552325-16-3 Molecular Weight 397.48 Purity 0.98 Storage Store at -20°C Synonyms A 443654; A443654 Targets Akt IC50 160 pM (Ki) Molecular Formula C24H23N5O Chemical Name (2S)-1-(1H-indol-3-yl)-3-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxypropan-2-amine Solubility Soluble in DMSO 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 552325-16-3 Basic Info-
Product Name:
A-443654
Other Name:A 443654;A-443654;A443654;(2s)-1-(1h-Indol-3-Yl)-3-{[5-(3-Methyl-1h-Indazol-5-Yl)pyridin-3-Yl]oxy}propan-2-Amine;(S)-1-(1H-Indol-3-yl)-3-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxypropan2-amine;(S)-1-(5-(3-Methyl-1H-indazol-5-yl)pyridin-3-yloxy)-3-(1H-indol-3-yl)propan-2-amine;L20
CAS No.:552325-16-3
Molecular Formula:C24H23N5O
InChIKeys:YWTBGJGMTBHQTM-IBGZPJMESA-N
Molecular Weight:397.47232
Exact Mass:397.190247
DSSTox ID:DTXSID20436347
Categories:
Characteristics-
PSA:
92.61000
XLogP3:3.65
Density:1.3±0.1 g/cm3
Boiling Point:722℃
Flash Point:390℃
Refractive Index:1.722
Hazard IdentificationClassification of the substance or mixture
no data available
GHS label elements, including precautionary statements
Pictogram(s) no data available Signal word no data available
Hazard statement(s) no data available
Precautionary statement(s) Prevention no data available
Response no data available
Storage no data available
Disposal no data available
Other hazards which do not result in classification
no data available
Handling and StoragePrecautions for safe handling
Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.
Conditions for safe storage, including any incompatibilities
Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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