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Cat. No.: HY-112602

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PI3K/mTOR Inhibitor-1

1 Cited Publications

고객리뷰

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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CAS No.: 1949802-49-6
화학식: C₁₈H₂₂FN₅O₃S
분자량:407.46

보관:

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

Data Sheet (276 KB)

PI3K/mTOR Inhibitor-1 Chemical Structure

CAS No.: 1949802-49-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

PI3Kα

20 nM (IC₅₀)

PI3Kβ

376 nM (IC₅₀)

PI3Kγ

204 nM (IC₅₀)

PI3Kδ

46 nM (IC₅₀)

mTOR

186 nM (IC₅₀)

All PI3K Isoforms :

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	0.108 μM Compound: 26	Cytotoxicity against HUVEC after 72 hrs by MTT assay Cytotoxicity against HUVEC after 72 hrs by MTT assay	[PMID: 30034607]
MCF7	IC₅₀	0.011 μM Compound: 26	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	[PMID: 30034607]
T47D	IC₅₀	0.03 μM Compound: 26	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	[PMID: 30034607]

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].

MedChemExpress (MCE) 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.

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].

MedChemExpress (MCE) 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.

Chemical Information

CAS No. 1949802-49-6
분자량 407.46
화학식 C₁₈H₂₂FN₅O₃S
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

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

Publications (1)

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Journal Impact Factor

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

PI3K/mTOR Inhibitor-1

1 Cited Publications

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
순도&문서
References

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PI3K/mTOR Inhibitor-1

Publications Citing Use of MedChemExpress (MCE) PI3K/mTOR Inhibitor-1

All PI3K Isoforms

All mTOR Isoforms

Biological Activity

Chemical Information

Publications (1)

순도&문서

References

Calculators

Help & FAQs

PI3K/mTOR Inhibitor-1 Related Classifications

HY-112602 Related Classifications