Find Tic10 Inhibitor, Cct128930 Inhibitor, A-674563 Inhibitor on Industry Directory, Reliable Manufacturer/Supplier/Factory from China.

Inquiry Basket (0)
Home > Products > PI3K/Akt/mTOR > Akt Inhibitor > TIC10 41276-02-2

TIC10 41276-02-2

Product Description

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight: 386.49 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. Phase 1/2.


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.


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.





Animal Models Female athymic nu/nu mice
Formulation DMSO
Dosages 25, 50, 100 mg/kg
Administration Intraperitoneal/oral


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)










Chemical Information




Molecular Weight (MW) 386.49
Formula

C24H26N4O

CAS No. 41276-02-2

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms ONC201



Solubility (25°C) * In vitro DMSO 11 mg/mL (28.46 mM)
Water <1 mg/mL (
Ethanol <1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.




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)-







Molarity Calculator
Dilution Calculator
Molecular Weight Calculator

Contact us if you need more details on TIC10 41276-02-2. We are ready to answer your questions on packaging, logistics, certification or any Other aspects about 41276-02-2 TIC10、41276-02-2. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : PI3K/Akt/mTOR > Akt Inhibitor