PI3K/mTOR Inhibitor-12
PI3K/mTOR Inhibitor-12 is a potent, orally active and selective PI3K/mTOR inhibitor with IC50 values of 0.06 nM and 3.12 nM for PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-12 has antitumor activity. PI3K/mTOR Inhibitor-12 has lower liver toxicity.
For research use only. We do not sell to patients.
- CAS No.: 2891692-83-2
- Formula: C27H27F2N9O4S
- Molecular Weight:611.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PI3Kα 0.06 nM (IC50) |
mTOR 3.12 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.54 μM
Compound: 42
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 36586298] |
| HT-29 | IC50 |
0.09 μM
Compound: 42
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Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 36586298] |
| HUVEC | IC50 |
0.68 μM
Compound: 42
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Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 36586298] |
| LoVo | IC50 |
0.54 μM
Compound: 42
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Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 36586298] |
| PC-3 | IC50 |
0.07 μM
Compound: 42
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Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 36586298] |
PI3K/mTOR Inhibitor-12 (compound 48; 72 h) inhibits cancer cells growth with IC50 values of 0.07, 0.09, 0.54, 0.54, and 0.68 μM for PC-3, HT-29,HCT116, LOVO, and HUVEC cells, respectively[1].
PI3K/mTOR Inhibitor-12 (0.25-1 μM; 12-48 h; HCT116 and HT-29 cells) inhibits the activation of PI3K and mTOR in the cellular context[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 and HT-29 cells
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Concentration:0.25, 0.5, and 1 μM
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Incubation Time:12, 24, and 48 hours
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Result:Inhibited the expression levels of AKT, p70S6K and their phosphorylated forms in a dose- and time-dependent manner.
PI3K/mTOR Inhibitor-12 (1 and 5 mg/kg; i.v. and p.o.; male SD rats) has fast plasma clearance (1428 mL/h/kg) and short T1/2 (2.33 h) and the AUC0-∞ is 1356 h*ng/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116 xenografts in female BALB/c nude mice[1]
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Dosage:20 mg/kg
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Administration:Oral administration, daily, for 14 days
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Result:Reduced the growth of HCT116 tumors, and the tumor growth inhibition (TGI) was 73.33%.
Had lower liver toxicity of HCT116 xenografts in female BALB/c nude mice.
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Animal Model:Male SD rats[1]
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Dosage:1 and 5 mg/kg
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Administration:Intravenous injection (1 mg/kg) and oral administration (5 mg/kg)
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Result:
1.19 Parameter I.V. (1 mg/kg) Parameter P.O. (5 mg/kg) T1/2 (h) 0.6 T1/2 (h) 2.33 CL (mL/h/kg) 1428 Cmax (ng/mL) 1218 Vdss (mL/Kg) 528 AUC0-∞ (h*ng/mL) 1356 AUC0-∞ (h*ng/mL) 760 F% 33.1
Chemical Information
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CAS No. 2891692-83-2
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Molecular Weight 611.62
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Formula C27H27F2N9O4S
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SMILES
O=S(C1=CC=C(F)C=C1F)(NC2=CC(C3=NN4C(C=C3)=NC=C4C5=CN(CCCN6CCOCC6)N=N5)=CN=C2OC)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3K/mTOR Inhibitor-12 Related Classifications
HY-152238 Related Classifications
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