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> Sapanisertib [1224844-38-5]

Sapanisertib [1224844-38-5]

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Referencia HY-13328-10mg

embalaje : 10mg

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Descripciòn

Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.

IC50 & Target[2]

mTOR

1 nM (IC50)

mTORC1

 

mTORC2

 

PI3Kα

219 nM (IC50)

PI3Kγ

221 nM (IC50)

PI3Kδ

230 nM (IC50)

PI3Kβ

5.293 μM (IC50)

Autophagy

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.174 μM
Compound: MLN0128; INK128
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
Bel-7402 IC50
>100 μM
Compound: MLN0128; INK128
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
CNE-2 IC50
0.101 μM
Compound: MLN0128; INK128
Antiproliferative activity against human CNE-2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human CNE-2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
HCT-116 IC50
0.048 μM
Compound: MLN0128; INK128
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
HeLa IC50
0.036 μM
Compound: MLN0128; INK128
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
Hep 3B2 IC50
4.43 μM
Compound: MLN0128; INK128
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
HepG2 IC50
1.73 μM
Compound: 5; MLN0128
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
[PMID: 37421709]
HepG2 IC50
2.13 μM
Compound: MLN0128; INK128
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
HL-60 IC50
0.16 μM
Compound: 5; MLN0128
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
[PMID: 37421709]
Huh-7 IC50
0.007 μM
Compound: MLN0128; INK128
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
HUVEC IC50
>10 μM
Compound: 5; MLN0128
Cytotoxicity against HUVEC assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
Cytotoxicity against HUVEC assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
[PMID: 37421709]
L02 IC50
0.28 μM
Compound: MLN0128; INK128
Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 34509167]
MCF7 IC50
0.053 μM
Compound: MLN0128; INK128
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
MCF7 IC50
1.23 μM
Compound: 5; MLN0128
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 70 hrs by CCK-8 assay
[PMID: 37421709]
MDA-MB-231 IC50
0.031 μM
Compound: MLN0128; INK128
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
PLC-PRF-5 IC50
6.63 μM
Compound: MLN0128; INK128
Antiproliferative activity against human PLC-PRF-5 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human PLC-PRF-5 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
SK-HEP1 IC50
0.008 μM
Compound: MLN0128; INK128
Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
SNU-423 IC50
0.015 μM
Compound: MLN0128; INK128
Antiproliferative activity against human SNU-423 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human SNU-423 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
[PMID: 34509167]
In Vitro

Sapanisertib (INK-128) exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases[1].
Sapanisertib (INK-128) selectively decreases the expression of YB1, MTA1, vimentin and CD44 at the protein but not transcript level in PC3 cells. Sapanisertib (INK-128) decreases the invasive potential of PC3 prostate cancer cells. Furthermore, Sapanisertib (INK-128) inhibits cancer cell migration starting at 6 h of treatment, precisely correlating with when decreases in the expression of pro-invasion genes are evident, but preceding any changes in the cell cycle or overall global protein synthesis[2].

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

Sapanisertib Related Antibodies

Solvente y solubilidad
In Vitro: 

DMSO : 55 mg/mL (177.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2328 mL 16.1640 mL 32.3279 mL
5 mM 0.6466 mL 3.2328 mL 6.4656 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Pureza y Documentación
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