Sapanisertib (Synonyms: INK-128; MLN0128; TAK-228)

Name: Sapanisertib
Brand: MedChemExpress
SKU: HY-13328
Rating: 5.0 (40 reviews)

Cat. No.: HY-13328 Purity: 99.49%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

Sapanisertib Chemical Structure

CAS No. : 1224844-38-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 106	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 106	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 40 publication(s) in Google Scholar

36 Publications Citing Use of MCE Sapanisertib

: Sapanisertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617. [Abstract]; Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

: Sapanisertib purchased from MedChemExpress. Usage Cited in: Oncogene. 2015 Mar 26;34(13):1729-35. [Abstract]; INK-128 ablates phosphorylation of the mTORC1 substrates, 4E-BP1 and S6K.

: Sapanisertib purchased from MedChemExpress. Usage Cited in: J Virol. 2014 Oct;88(20):11872-85. [Abstract]; Confocal analysis of MTA1 (red) and β-catenin (green) expression in CNE-1-LMP2A cells treated with Rapamycin (50 nM) or INK-128 (200 nM) for 24 h. The scale bar represents 10 μm. Immunofluorescence analysis of MTA1 and β-catenin expression reveals that MTA1 is decreased and β-catenin is maintained in the cytoplasm when the cells are treated with INK-128.

: Sapanisertib purchased from MedChemExpress. Usage Cited in: J Virol. 2014 Oct;88(20):11872-85. [Abstract]; Representative Western blot from two independent experiments of p-Akt, p-mTOR, mTOR, p-4EBP1, 4EBP1, eIF4E, c-myc, and MTA1 genes in CNE-1-LMP2A cells treated with Rapamycin (50 nM) or INK-128 (200 nM) for 24 h. The quantification of the Western blot signals are analyzed.

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mTOR mTORC1 mTORC2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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	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]
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]
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]
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.

In Vivo

In a ZR-75-1 breast cancer xenograft model, Sapanisertib (INK-128) shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day^[1].
4EBP1 and p70S6K1/2 phosphorylation is completely restored to wild-type levels after treatment with INK128 in PtenL/L mice. Sapanisertib (INK-128) treatment results in a 50% decrease in prostatic intraepithelial neoplasia (PIN) lesions in PtenL/L mice and induces programmed cell death in multiple cancer cell lines in mice^[2].

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

Clinical Trial

Molecular Weight

309.33

Formula

C₁₅H₁₅N₇O

CAS No.

1224844-38-5

Appearance

Solid

Color

White to off-white

SMILES

NC1=NC=NC2=C1C(C3=CC4=C(C=C3)OC(N)=N4)=NN2C(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.66%

Select Batch:

Data Sheet (283 KB) SDS (251 KB)

COA (256 KB) HNMR (266 KB) LCMS (97 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]

Cell Assay ^[2]	PC3 cells are treated with the appropriate drug for 48 h, and proliferation is measured using CellTiter-Glo Luminescent reagent. The concentration of Sapanisertib (INK-128) necessary to achieve inhibition of cell growth by 50% (IC₅₀) is calculated using concentrations ranging from 20.0 μM to 0.1 nM (12-point curve). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Nude mice are inoculated subcutaneously in the right subscapular region with 5×10⁶ MDA-MB-361 cells. After tumours reach a size of 150-200 mm³, mice are randomLy assigned into vehicle control or treatment groups. Sapanisertib (INK-128) is formulated in 5% polyvinylpropyline, 15% NMP, 80% water and administered by oral gavage at 0.3 mg/kg and 1 mg/kg daily. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.2328 mL	16.1640 mL	32.3279 mL	80.8198 mL
	5 mM	0.6466 mL	3.2328 mL	6.4656 mL	16.1640 mL
	10 mM	0.3233 mL	1.6164 mL	3.2328 mL	8.0820 mL
	15 mM	0.2155 mL	1.0776 mL	2.1552 mL	5.3880 mL
	20 mM	0.1616 mL	0.8082 mL	1.6164 mL	4.0410 mL
	25 mM	0.1293 mL	0.6466 mL	1.2931 mL	3.2328 mL
	30 mM	0.1078 mL	0.5388 mL	1.0776 mL	2.6940 mL
	40 mM	0.0808 mL	0.4041 mL	0.8082 mL	2.0205 mL
	50 mM	0.0647 mL	0.3233 mL	0.6466 mL	1.6164 mL
	60 mM	0.0539 mL	0.2694 mL	0.5388 mL	1.3470 mL
	80 mM	0.0404 mL	0.2020 mL	0.4041 mL	1.0102 mL
	100 mM	0.0323 mL	0.1616 mL	0.3233 mL	0.8082 mL

Sapanisertib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sapanisertib1224844-38-5INK-128 MLN0128 TAK-228INK128INK 128MLN0128MLN 0128MLN-0128TAK228TAK 228TAK-228mTORAutophagyMammalian target of RapamycinInhibitorinhibitorinhibit

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Sapanisertib (Synonyms: INK-128; MLN0128; TAK-228)

Customer Review

Sapanisertib Related Antibodies

36 Publications Citing Use of MCE Sapanisertib

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Sapanisertib Related Antibodies

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Complete Stock Solution Preparation Table

Sapanisertib Related Classifications

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