PI3K/mTOR Inhibitor-1

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PI3K/mTOR Inhibitor-1 

PI3K/mTOR Inhibitor-1 是一种有效的，口服生物可利用的双重 PI3K/mTOR 抑制剂，抑制 PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ 和 mTOR，IC50 分别为 20/376/204/46 nM 和 186 nM。具有抗肿瘤活性。

PI3K/mTOR Inhibitor-1

PI3K/mTOR Inhibitor-1 Chemical Structure

CAS No. : 1949802-49-6

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生物活性

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[1]. Antitumor activity[1].

IC50 & Target[1]

PI3Kα

20 nM (IC50)

PI3Kβ

376 nM (IC50)

PI3Kγ

204 nM (IC50)

PI3Kδ

46 nM (IC50)

mTOR

186 nM (IC50)

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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
Concentration: 0.046-10 µM
Incubation Time: 72 hours
Result: Inhibited HT-29 cells proliferation with an IC50 of 0.163 μM.

体内研究
(In Vivo)

PI3K/mTOR Inhibitor-1 (Compound 26) produces 54.4% tumor growth inhibition (TGI) with daily oral doses of 3.75 mg/kg for 27 days. The 7.5 mg/kg group of PI3K/mTOR Inhibitor-1 displays more significant TGI (72.9%). All animals survive after 27-day treatment, whereas 15% weigh loss is observed in PI3K/mTOR Inhibitor-1, 7.5 mg/kg group[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c nu/nu mice with HT-29 colorectal carcinoma xenograft mouse model carrying the PIK3CA P449T mutation[1]
Dosage: 3.75 and 7.5 mg/kg
Administration: Oral gavage daily for 27 days
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.

分子量

407.46

Formula

C18H22FN5O3S
CAS 号

1949802-49-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Shen S, et al. Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines. ACS Med Chem Lett. 2018 Jun 25;9(7):719-724.

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