PI3K/mTOR Inhibitor-1
Based on 1 publication(s) in Google Scholar
PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity.
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- No. CAS: 1949802-49-6
- Fòrmula: C18H22FN5O3S
- Peso molecular:407.46
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Almacenamiento:
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Actividad biológica
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PI3Kα 20 nM (IC50) |
PI3Kβ 376 nM (IC50) |
PI3Kγ 204 nM (IC50) |
PI3Kδ 46 nM (IC50) |
mTOR 186 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HUVEC | IC50 |
0.108 μM
Compound: 26
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Cytotoxicity against HUVEC after 72 hrs by MTT assay
Cytotoxicity against HUVEC after 72 hrs by MTT assay
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[PMID: 30034607] |
| MCF7 | IC50 |
0.011 μM
Compound: 26
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Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay
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[PMID: 30034607] |
| T47D | IC50 |
0.03 μM
Compound: 26
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Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay
Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay
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[PMID: 30034607] |
PI3K/mTOR Inhibitor-1 (Compound 26) also exhibits potent functional suppression of AKT phosphorylation (IC50=196 nM)[1].
PI3K/mTOR Inhibitor-1 (0.046-10 µM, 72 hours) exhibits excellent antiproliferative effects on a panel of cancer cells. PI3K/mTOR Inhibitor inhibits A431, A549, PC3, MDA-MB-361, SW480, ES-2, HT29, SK-OV-3, HCT116 , G401 , BT20 ,DLD1 HCC827, H1650, H460, Farage, H820, HCT15, H358, Colo-205, PC9, H1975, WSU-DLCL2, HT, A2780, SU-DHL-10, Toledo,SU-DHL-6, DB, and Pfeiffer cells with IC50s of 0.188, 0.104, 0.063, 0.085, 0.534, 0.179, 0.163, 0.135, 0.308, 0.113, 0.729, 0.264, 0.287, 1.662, 0.611, 0.202, 0.365, 0.104, 0.098, 0.109, 0.237, 0.136, 0.145, 0.090, 0.251 0.215, 0.269, 0.111 0.062, and 0.061 µM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87-MG, A431, MCF-7, PC3, A549, MDA-MB-361, SW480, ES-2, HT29, SK-OV-3, HCT116, G401, BT20, DLD1, HCC827, H1650, H460, Farage, H820, HCT15, H358, Colo-205, PC9, H1975, WSU-DLCL2, HT, A2780, SU-DHL-10, Toledo, SU-DHL-6, DB, Pfeiffer cells
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Concentration:0.046-10 µM
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Incubation Time:72 hours
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Result:Inhibited HT-29 cells proliferation with an IC50 of 0.163 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c nu/nu mice with HT-29 colorectal carcinoma xenograft mouse model carrying the PIK3CA P449T mutation[1]
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Dosage:3.75 and 7.5 mg/kg
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Administration:Oral gavage daily for 27 days
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Result:Tumor growth inhibition (TGI) was 54.4% and 72.9% for daily oral doses of 3.75 mg/kg and 7.5 mg/kg for 27 days, respectively.
Chemical Information
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No. CAS 1949802-49-6
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Peso molecular 407.46
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Fòrmula C18H22FN5O3S
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SMILES
NC1=CC(F)=C(C2=CC(C3(CC3)S(=O)(C)=O)=NC(N4[C@@H](C)COCC4)=N2)C=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Environ Pollut
BPA modulates the WDR5/TET2 complex to regulate ERβ expression in eutopic endometrium and drives the development of endometriosis. [Abstract]2021 Jan 1;268(Pt B):115748. PMID: 33022573
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3K/mTOR Inhibitor-1 Related Classifications
HY-112602 Related Classifications
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