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 TIC10 Cat No CEI-0896 Description TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Alias TRAIL-inducing Compound 10 CAS No 41276-02-2 Molecular Weight 386.49 Storage 2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO. Synonyms TRAIL-inducing Compound 10 Targets Akt, ERK Molecular Formula C24H26N4O Chemical Name Imidazo[1,2-a]pyrido[4,3-d]pyrimidin-5(3H)-one, 2,6,7,8,9,10-hexahydro-10-[(2-methylphenyl)methyl]-7-(phenylmethyl)- Solubility DMSO mg/mL; Water mg/mL; Ethanol mg/mL In vitro TIC10 causes a dose-dependent increase in TRAIL mRNA and induces TRAIL protein localization on the cell surface of several cancer cell lines in a p53-independent manner. TIC10 has broad-spectrum activity against multiple malignancies in vitro and induces an increase in sub-G1 DNA content suggestive of cell death in TRAIL-sensitive HCT116 p53−/− cells, but does not alter the cell cycle profiles of normal fibroblasts at equivalent doses. TIC10 decreases the clonogenic survival of cancer cell lines and spares normal fibroblasts. TIC10 increases the percentage of sub-G1 DNA in cancer cells in a p53-independent and Bax-dependent manner, as previously reported for TRAIL-mediated apoptosis. TIC10-induced TRAIL up-regulation is Foxo3a-dependent, which also up-regulates TRAIL death receptor DR5 among other targets, potentially allowing for sensitization of some TRAIL-resistant tumor cells. TIC10 inactivates kinases Akt and extracellular signal–regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. TIC10 is an efficacious antitumor therapeutic agent that acts on tumor cells and their microenvironment to enhance the concentrations of the endogenous tumor suppressor TRAIL. In vivo TIC10 and TRAIL treatment causes tumor regression in the HCT116 p53−/− xenograft to a comparable extent when both are administered as multiple doses. TIC10 also induces regression of MDA-MB-231 human triple-negative breast cancer xenografts, whereas TRAIL-treated tumors progressed. In DLD-1 colon cancer xenografts, TIC10 induces tumor stasis at 1 week after treatment, whereas TRAIL-treated tumors progresses after a single dose. A single dose of TIC10 also induces a sustained regression of the SW480 xenograft and is equally effective when delivered by intraperitoneal or oral route, suggesting favorable oral bioavailability for TIC10. TIC10 causes tumor-specific cell death by TRAIL-mediated direct and bystander effects. TIC10 is an effective antitumor agent against orthotopic human glioblastoma multiforme tumors. category Inhibitors(c1514) cas_num 41276-02-2 Basic Info-
Product Name:
7-benzyl-10-(2-Methylbenzyl)-2,6,7,8,9,10-hexahydroiMidazo[1,2-a]pyrido[4,3-d]pyriMidin-5(3H)-one
Other Name:7-benzyl-10-(2-Methylbenzyl)-2,6,7,8,9,10-hexahydroiMidazo[1,2-a]pyrido[4,3-d]pyriMidin-5(3H)-one;TIC 10;TIC10;TIC-10;2,6,7,8,9,10-Hexahydro-10-[(2-methylphenyl)methyl]-7-(phenylmethyl)-imidazo[1,2-a]pyrido[4,3-d]pyrimidin-5(3H)-one;NSC 350625;ONC201,NSC 350625;Imidazo[1,2-a]pyrido[4,3-d]pyrimidin-5(3H)-one, 2,6,7,8,9,10-hexahydro-10-[(2-methylphenyl)methyl]-7-(phenylmethyl)-
CAS No.:41276-02-2
Molecular Formula:C24H26N4O
InChIKeys:RSAQARAFWMUYLL-UHFFFAOYSA-N
Molecular Weight:386.48944
Exact Mass:386.211
EC Number:-0
DSSTox ID:DTXSID30319793
Categories:
Characteristics-
PSA:
39.2
XLogP3:2.3
Appearance:white to beige
Density:1.24g/cm3
Boiling Point:559.7ºC at 760mmHg
Flash Point:292.3ºC
Refractive Index:1.672
Water Solubility:DMSO: soluble 2mg/mL, clear (warmed)
Storage Conditions:2-8°C
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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Country Product Purchase Quantity Date Posted Post an enquiry for this product