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Reagents and instruments for immunology, cell biology and molecular biology.

Sapanisertib [1224844-38-5]

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Cat# HY-13328-5mg

Size : 5mg

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Description

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.

Solvent & Solubility

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
10 mM	0.3233 mL	1.6164 mL	3.2328 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation

Purity: 99.88%

Data Sheet (283 KB) SDS (396 KB)

COA (256 KB) HNMR (147 KB) RP-HPLC (222 KB) MS (73 KB)

Handling Instructions (2659 KB)

References

[1]. Liu A, et al. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55. [Content Brief]

[2]. Hsieh AC, et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature. 2012 Feb 22;485(7396):55-61. [Content Brief]

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Sapanisertib [1224844-38-5]

Cat# HY-13328-5mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

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