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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1949802-49-6
- 分子式: C18H22FN5O3S
- 分子量:407.46
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 PI3K/mTOR Inhibitor-1
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生物活性
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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.
化学情報
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CAS 番号 1949802-49-6
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分子量 407.46
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PI3K/mTOR Inhibitor-1 関連分類
HY-112602 関連分類
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