AT13148 1056901-62-2
Product Description
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Molecular Weight: 313.78 AT13148 is an oral, ATP-competitive, Multi-AGC Kinase Inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.
AT13148,
as a multi-AGC kinase inhibitor, potently inhibits proliferation with
GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell
lines with deregulation of PI3K-AKT-mTOR or RAS-RAF pathways. In
PTEN-deficient MES-SA cells, AT13148 also inhibits AKT and p70S6K
signaling.AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and
p70S6K AGC kinases, and subsequently exhibits marked antitumor effects
in human tumor xenografts.
Cell Assay: [1]
Animal Study: [1]
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.
Chemical Information
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Contact us if you need more details on AT13148 1056901-62-2. We are ready to answer your questions on packaging, logistics, certification or any other aspects about 1056901-62-2 AT13148、1056901-62-2. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight: 313.78 AT13148 is an oral, ATP-competitive, Multi-AGC Kinase Inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.
AT13148,
as a multi-AGC kinase inhibitor, potently inhibits proliferation with
GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell
lines with deregulation of PI3K-AKT-mTOR or RAS-RAF pathways. In
PTEN-deficient MES-SA cells, AT13148 also inhibits AKT and p70S6K
signaling.AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and
p70S6K AGC kinases, and subsequently exhibits marked antitumor effects
in human tumor xenografts.
In vitro kinase assays | AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme. |
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Cell Assay: [1]
Cell lines | MES-SA, MES-SA/Dx5, BT474, HCT-116, A549, PC3, SK-BR-3, MCF7, U87MG, MDA-MB-468, DU-145, and SK-OV-3 cell lines |
---|---|
Concentrations | ~10 μM |
Incubation Time | 72 hours or 96 hours |
Method | Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay. |
Animal Study: [1]
Animal Models | Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts |
---|---|
Formulation | 10% DMSO, 1% Tween-20, and 89% saline |
Dosages | ~50 mg/kg |
Administration | p.o. |
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) | 313.78 |
---|---|
Formula | C17H16ClN3O |
CAS No. | 1056901-62-2 |
Storage | 3 years -20℃Powder |
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6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | N/A |
Chemical Name | (S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol |
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Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on AT13148 1056901-62-2. We are ready to answer your questions on packaging, logistics, certification or any other aspects about 1056901-62-2 AT13148、1056901-62-2. 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
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