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  3. PI3K/mTOR Inhibitor-1

PI3K/mTOR Inhibitor-1 

Cat. No.: HY-112602
Handling Instructions

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.

For research use only. We do not sell to patients.

PI3K/mTOR Inhibitor-1 Chemical Structure

PI3K/mTOR Inhibitor-1 Chemical Structure

CAS No. : 1949802-49-6

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Description

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)

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].

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.
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].

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.
Storage

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

References
Molecular Weight

407.46

Formula

C₁₈H₂₂FN₅O₃S

CAS No.

1949802-49-6

SMILES

NC1=CC(F)=C(C2=CC(C3(CC3)S(=O)(C)=O)=NC(N4[[email protected]@H](C)COCC4)=N2)C=N1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PI3K/mTOR Inhibitor-1
Cat. No.:
HY-112602
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PI3K/mTOR Inhibitor-1

Cat. No.: HY-112602