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Cat. No.: HY-161509

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PT-88

PT-88 is a potent and selective ATP-competitive mTOR kinase inhibitor, IC₅₀ = 1.2 nM. PT-88 inhibits both mTORC1 and mTORC2 and blocks the phosphorylation of their downstream proteins (such as p70S6K, 4EBP1, and Akt), thereby inducing cancer cell cycle arrest, autophagy, and apoptosis. PT-88 can be used for research on human breast cancer.

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CAS No.: 2803307-04-0
화학식: C₃₀H₃₁N₇O₅
분자량:569.61

보관:

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

Data Sheet (279 KB)

PT-88 Chemical Structure

CAS No.: 2803307-04-0

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

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

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

mTOR

1.2 nM (IC₅₀)

TORC1

mTORC2

p70S6K

All mTOR Isoforms :

All Akt Isoforms :

All Ribosomal S6 Kinase (RSK) Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	0.74 μM	Cytotoxicity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by CCK8 assay. Cytotoxicity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.	38661655
MDA-MB-231	IC₅₀	2.29 μM	Cytotoxicity against human MDA-MB-231 cells assessed as viability reduction incubated 48 hrs by CCK8 assay. Cytotoxicity against human MDA-MB-231 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.	38661655
HepG2	IC₅₀	3.46 μM	Cytotoxicity against human HepG2 cells assessed as viability reduction incubated 48 hrs by CCK8 assay. Cytotoxicity against human HepG2 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.	38661655
HeLa	IC₅₀	10.27 μM	Cytotoxicity against human HeLa cells assessed as viability reduction incubated 48 hrs by CCK8 assay. Cytotoxicity against human HeLa cells assessed as viability reduction incubated 48 hrs by CCK8 assay.	38661655
HCT-116	IC₅₀	2.24 μM	Cytotoxicity against human HCT116 cells assessed as viability reduction incubated 48 hrs by CCK8 assay. Cytotoxicity against human HCT116 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.	38661655
CNE-2	IC₅₀	2.13 μM	Cytotoxicity against human CNE2 cells assessed as viability reduction incubated 48 hrs by CCK8 assay. Cytotoxicity against human CNE2 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.	38661655
L02	IC50	11.56 μM	Cytotoxicity against human L02 cells assessed as viability reduction incubated 48 hrs by CCK8 assay. Cytotoxicity against human L02 cells assessed as viability reduction incubated 48 hrs by CCK8 assay.	38661655

In Vitro

Anti-cancerApoptosisCell Cycle RegulationAutophagyOthers

Anti-cancer

PT-88 (increasing concentrations; 48 h) inhibits MCF-7 cell viability with IC₅₀ 0.74 μM and shows lower potency in MDA-MB-231, HepG2, HeLa, HCT116, CNE2, and LO2 cells^[1].
PT-88 (1-10 μM; 24 h) suppresses mTORC1/mTORC2 downstream phosphorylation in MCF-7 cells^[1].
PT-88 (0.5-2 μM; 2 weeks) inhibits MCF-7 colony formation^[1].
PT-88 (1-2 μM; 24-48 h) reduces MCF-7 wound healing^[1].

Anti-cancer

Apoptosis

Cell Cycle Regulation

PT-88 (2.5-10 μM; 24 h) induces G2/M-phase arrest in MCF-7 cells^[1].

Anti-cancer

Autophagy

PT-88 (0.1-10 μM; 24 h) induces autophagy markers in MCF-7 cells^[1].

Others

PT-88 is a potent mTOR inhibitor with IC₅₀ 1.2 nM and >10,000 nM IC₅₀ against PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ^[1].
PT-88 (up to 10 μM) does not inhibit CYP1A2, CYP2C9, CYP2C19, CYP2D6, or CYP3A-M^[1].
PT-88 has hERG IC₅₀ >30 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

1, 10 μM
Incubation Time:

24 h
Result:

Phosphorylation of p70S6K (T389), 4EBP1 (T37/46), and Akt (S473) was extensively prevented at 1 and 10 μM.

Cell Proliferation Assay^[1]

Cell Line:

MCF-7 cells
Concentration:

0.5, 1, 2 μM
Incubation Time:

2 weeks
Result:

MCF-7 colony formation was significantly inhibited at 0.5, 1, and 2 μM.

Cell Migration Assay ^[1]

Cell Line:

MCF-7 cells
Concentration:

1, 1.5, 2 μM
Incubation Time:

24 and 48 h
Result:

MCF-7 migration was inhibited in a concentration-dependent manner at 24 and 48 h.

Cell Cycle Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

2.5, 5, 10 μM
Incubation Time:

24 h
Result:

With increasing concentration, the G2/M-phase fraction increased from 27.90% to 48.90%, and the S-phase fraction decreased.

Apoptosis Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

2.5, 5, 10 μM
Incubation Time:

24 h
Result:

Total apoptotic cells were 18.2%, 13.0%, and 21.4% at 2.5, 5, and 10 μM, respectively.

Cell Autophagy Assay^[1]

Cell Line:

MCF-7 cells
Concentration:

0.1, 1, 10 μM
Incubation Time:

24 h
Result:

P62 decreased in a concentration-dependent manner; LC3I-to-LC3II conversion increased, with the increased effect higher at 1 μM.

Parmacokinetics

Species	Dose	Route	AUC_0-24	AUC_inf	T_1/2	C_max
Mice^[1]	5 mg/kg	i.v.	3782 μg/L·h	3783 μg/L·h	2.8 h	11852 μg/L

In Vivo

Anti-cancer

PT-88 (20 mg/kg; i.v.; once every other day for a total of 10 doses; continuous observation for 19 days) shows significant inhibition of tumor growth in the MCF-7 xenograft female nude mouse model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude (female, 6 weeks old)^[1]
Dosage:

20 mg/kg
Administration:

i.v.; once every other day for a total of 10 doses; continuous observation for 19 days
Result:

Resulted in a tumor growth inhibition (TGI) value of 45.6%.
Had high biosafety profiles.

Related Protocols :

Chemical Information

CAS No. 2803307-04-0
분자량 569.61
화학식 C₃₀H₃₁N₇O₅
SMILES

O=C(NC1=CC=C(C2=NC(N3C4COCC3CC4)=NC(N5[C@@H]6COC[C@H]5CC6)=N2)C=C1)NC7=CC8=C(C=C7)C(OC8)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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]. Sun Q, et al. Design, Synthesis, Formulation, and Bioevaluation of Trisubstituted Triazines as Highly Selective mTOR Inhibitors for the Treatment of Human Breast Cancer. Journal of medicinal chemistry. 2024 May 09;67(9):7330-7358. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

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

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

PT-88

All mTOR Isoforms

All Akt Isoforms

All Ribosomal S6 Kinase (RSK) Isoforms