Cat. No.: HY-13328

Sapanisertib

Name: Sapanisertib
Brand: MedChemExpress
SKU: HY-13328
Price: 96.00 USD
Availability: InStock
Rating: 5 (56 reviews)

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

56 Cited Publications

Customer Review

Based on 56 publication(s) in Google Scholar

Sapanisertib (INK-128; MLN0128; TAK-228) is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.

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

Purity: 99.78%
CAS No.: 1224844-38-5
Formula: C₁₅H₁₅N₇O
Molecular Weight:309.33

Storage:

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

Sapanisertib Chemical Structure

CAS No.: 1224844-38-5

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (56)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]^[2]^[3]

mTORC1

mTORC2

p70S6K

Akt

HIF-1α

Collagen I

Collagen III

Wnt5A

All mTOR Isoforms :

All Akt Isoforms :

All ERK Isoforms :

All CDK Isoforms :

All Ribosomal S6 Kinase (RSK) Isoforms :

All HIF/HIF Prolyl-Hydroxylase Isoforms :

All Wnt Isoforms :

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) (200 nM; overnight) phosphate enhances glycolytic capacity and alters lipid metabolism in mESCs^[3].
Sapanisertib (INK-128) (10-100 nM; 18 h) phosphate impairs in vitro maturation, reduces the MII formation rate, and decreases mTOR expression in mouse germinal vesicle (GV) stage oocytes^[5].
Sapanisertib (40 nM; 4-24 h) phosphate inhibits mTOR and ERK pathway activation in WM3311, WM2032, WM853-2, and WM858 human skin melanoma cell lines^[1].
Sapanisertib (1 nM; 72 h) phosphate inhibits TGF-β1 (HY-P78168)-induced epithelial-mesenchymal transition in A549 cells^[2].
Sapanisertib (INK-128) (3 nM-3 µM; 96 h) phosphate inhibits cell growth and synergizes with ABT-737 (HY-50907) to induce cell death in patient-derived xenograft (PDX) cell models derived from HGS-OvCa^[4].
Sapanisertib (10 nM; 24 h) phosphate induces apoptosis in M1 and M5 canine melanoma cell lines^[1].
Sapanisertib (0.125 nM-10 μM; 72 h) phosphate potently reduces the viability of canine mucosal melanoma cell lines (UCDK9M1, UCDK9M2, UCDK9M3, UCDK9M5, Jones) and human cutaneous melanoma cell lines (WM3311, WM2032, WM853-2, WM858), with IC₅₀ values ranging from 10 nM to 100 nM; furthermore, it exhibits synergistic effects with Trametinib (HY-10999), further decreasing cell survival in most of these cell lines^[1].
Sapanisertib (INK-128) (200 nM; 24 h) phosphate induces a reversible diapause-like state in R1 (LL) and R1 (SS) mouse embryonic stem cells by inhibiting the mTORC1/2 signaling pathway and reducing the transcriptionally active epigenetic mark H₄K16ac^[3].
Sapanisertib (0.5-1 nM; 72 h) phosphate inhibits TGF-β1-induced L929 cell proliferation, and at 1 nM, it suppresses collagen deposition and Wnt5a/mTOR signaling pathway activation^[2].

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

Western Blot Analysis^[1]

Cell Line:

M1, M5, Jones, WM3311, WM2032, WM853-2, WM858 cells
Concentration:

40 nmol/L
Incubation Time:

4 h, 24 h
Result:

Inhibited the phosphorylation of p-AKT and the downstream effector p-S6, and altered the expression of cell cycle proteins (Cyclin B1) and apoptosis-related proteins (p-BAD).

Apoptosis Analysis^[1]

Cell Line:

M1, M5 cells
Concentration:

10 nM
Incubation Time:

24 h
Result:

Showed a trend toward inducing cell apoptosis.

Immunofluorescence^[2]

Cell Line:

A549 cells
Concentration:

1 nM
Incubation Time:

72 h
Result:

Prevented the TGF-β1-induced decrease in E-cadherin protein expression.

Western Blot Analysis^[2]

Cell Line:

A549 cells
Concentration:

1 nM
Incubation Time:

72 h
Result:

Suppressed the TGF-β1-induced increase in vimentin expression.

Cell Proliferation Assay^[2]

Cell Line:

L929 cells
Concentration:

0.5, 1 nM
Incubation Time:

72 h
Result:

Strongly inhibited the cell proliferation induced by TGF-β1 stimulation.

Western Blot Analysis^[2]

Cell Line:

L929 cells
Concentration:

1 nM
Incubation Time:

72 h
Result:

Significantly reduced the TGF-β1-induced overexpression of α-SMA, collagen I, and collagen III, and decreased the protein levels of Wnt5a, mTOR, HIF-1α, and p70S6K.

Western Blot Analysis^[3]

Cell Line:

mESCs (R1(LL) and R1(SS)) cells
Concentration:

200 nM
Incubation Time:

24 h
Result:

Downregulated the phosphorylation of mTOR complex targets (S6, 4EBP1, Akt) and decreased the epigenetic mark H4K16ac.

Cell Viability Assay^[4]

Cell Line:

HGS-OvCa PDX in vitro cultured cells (e.g., DF68, DF101, DF14)
Concentration:

0.003, 0.01, 0.03, 0.1, 0.3, 1, 3 µM
Incubation Time:

96 h
Result:

Exhibited a distinct cell growth inhibition effect and further reduced cell viability when combined with ABT-737.

Cell Cycle Analysis^[5]

Cell Line:

mouse germinal vesicle (GV) stage oocytes
Concentration:

10, 50, 100 nM
Incubation Time:

18 h
Result:

Reduced the overall maturation rate from the GV stage to the MII stage and caused abnormal morphological changes such as enlarged polar bodies and increased cytoplasmic granularity.

Immunofluorescence^[5]

Cell Line:

mouse oocytes
Concentration:

10, 50, 100 nM
Incubation Time:

18 h
Result:

Significantly reduced the expression of mTOR in MII stage oocytes, and abnormal spindle organization was observed.

In Vivo

Sapanisertib (INK-128) (2.0 mg/kg; p.o.; 3 times per week; for 28 days) phosphate slightly reduces thoracic metastatic tumor burden in a metastatic melanoma nude mouse model established by tail vein injection of an M1-derived subline^[1].
Sapanisertib (INK-128) (2.0-3.0 mg/kg; p.o.; daily or every other day; 3-21 days) phosphate monotherapy inhibits the growth of canine mucosal melanoma xenografts and PI3K/AKT/mTOR pathway activity, but induces compensatory ERK activation; when administered every other day or in combination with Trametinib, both tolerability and efficacy are improved^[1].
Sapanisertib (1 mg/kg; i.g.; daily administration; 14 days) phosphate attenuates pulmonary fibrosis, reduces collagen deposition, and improves pathological scores in a rat model of pulmonary fibrosis induced by intratracheal instillation of Bleomycin (HY-17565A)^[2].

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

Animal Model:

Sprague-Dawley (male, 8-9 weeks old, 180-200 g, bleomycin-induced pulmonary fibrosis model)^[2]
Dosage:

1 mg/kg
Administration:

i.g.; once daily; 14 days
Result:

Increased lung Hounsfield unit values compared to bleomycin-exposed alone rats.
Reduced pathological scores measured via H&E staining.
Decreased lung coefficient values.
Reduced pulmonary collagen deposition measured via Masson's trichrome staining.
Lowered Ashcroft scores.
Reduced hydroxyproline levels.
Decreased protein expression of collagen I and collagen III.
Blocked bleomycin-induced increases in Wnt5a, mTOR, HIF-1α, α-SMA, and p-p70S6K.
Reversed bleomycin-induced decreases in E-cadherin protein expression.

Animal Model:

nu/nu athymic nude mice (6- to 8-week-old female; experimental metastasis model via intravenous tail vein injection of M1-derived metastatic subline cells)^[1]
Dosage:

2.0 mg/kg
Administration:

p.o.; three times a week; 28 days
Result:

Reduced intrathoracic metastatic tumor burden compared with vehicle control, but was less effective than single-agent daily trametinib.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1224844-38-5
Appearance Solid
Molecular Weight 309.33
Formula C₁₅H₁₅N₇O
Color White to off-white
SMILES

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

INK-128; MLN0128; TAK-228
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

Publications (56)

All WBIF

Sort by:

Journal Impact Factor

Nature

Inhibition of mTOR induces a paused pluripotent state. [Abstract]

2016 Dec 1;540(7631):119-123. PMID: 27880763
Cell

mTOR activity paces human blastocyst stage developmental progression. [Abstract]

2024 Nov 14;187(23):6566-6583.e22. PMID: 39332412
Cell Stem Cell

Histone Acetyltransferase MOF Blocks Acquisition of Quiescence in Ground-State ESCs through Activating Fatty Acid Oxidation. [Abstract]

2020 Sep 3;27(3):441-458.e10. PMID: 32610040
Cell Stem Cell

The Transcriptionally Permissive Chromatin State of Embryonic Stem Cells Is Acutely Tuned to Translational Output. [Abstract]

2018 Mar 1;22(3):369-383.e8. PMID: 29499153
Nat Cell Biol

Chromosome mis-segregation triggers cell cycle arrest through a mechanosensitive nuclear envelope checkpoint. [Abstract]

2025 Jan;27(1):73-86. PMID: 39779939
Nat Cell Biol

FOXO1-mediated lipid metabolism maintains mammalian embryos in dormancy. [Abstract]

2024 Feb;26(2):181-193. PMID: 38177284
Cancer Res

Genome-Wide CRISPR Screening Reveals that mTOR Inhibition Initiates Ferritinophagy and Ferroptosis in Head and Neck Cancer. [Abstract]

2025 Jun 6. PMID: 40479615
Autophagy

African swine fever virus I10L protein inhibits autolysosome formation by disrupting RAB7-HOPS complex-dependent SNARE complex assembly. [Abstract]

2026 May 15:1-16. PMID: 42138513
Nat Commun

Codon bias imposes a targetable limitation on KRAS-driven therapeutic resistance. [Abstract]

2017 Jun 8:8:15617. PMID: 28593995

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 inhibitor MLN0128 (Sapanisertib).
Mol Cell

mTORC1 activity suppresses ferroptosis through a SCARB1-dependent HDL-tocopherol uptake pathway. [Abstract]

2026 Apr 16;86(8):1546-1559.e8. PMID: 41997112
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Sci Adv

Oxytocin induces embryonic diapause. [Abstract]

2025 Mar 7;11(10):eadt1763. PMID: 40043121
Sci Adv

MAPK6-AKT signaling promotes tumor growth and resistance to mTOR kinase blockade. [Abstract]

2021 Nov 12;7(46):eabi6439. PMID: 34767444
Sci Adv

TRIBE editing reveals specific mRNA targets of eIF4E-BP in Drosophila and in mammals. [Abstract]

2020 Aug 12;6(33):eabb8771. PMID: 32851185
Cell Death Dis

mTOR inhibition enhances the antitumor efficacy of pan-RAF-MEK blockade by inhibiting the ATF4-MTHFD2 pathway. [Abstract]

2026 May 6;17(1):600. PMID: 42091854
Nat Struct Mol Biol

TET activity safeguards pluripotency throughout embryonic dormancy. [Abstract]

2024 Oct;31(10):1625-1639. PMID: 38783076
Dev Cell

Metabolic Control over mTOR-Dependent Diapause-like State. [Abstract]

2020 Jan 27;52(2):236-250.e7. PMID: 31991105
Oncogene

The ShcA adaptor activates AKT signaling to potentiate breast tumor angiogenesis by stimulating VEGF mRNA translation in a 4E-BP-dependent manner. [Abstract]

2015 Mar 26;34(13):1729-35. PMID: 24837366

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.
Aging Cell

2026 Jan 20;25(2):e70352.
Cell Rep

Coordinated expression of retained introns and poison exons in renal cell carcinoma. [Abstract]

2025 Jul 17;44(8):115985. PMID: 40682778
Cell Rep

Enhanced bypass of PD-L1 translation reduces the therapeutic response to mTOR kinase inhibitors. [Abstract]

2023 Jul 4;42(7):112764. PMID: 37405918
Cell Syst

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]

2020 Jan 22;10(1):66-81.e11. PMID: 31812693
Mol Ther Nucleic Acids

2025 Dec 15.
Cancer Metab

Long-acting Erwinia chrysanthemi, Pegcrisantaspase, induces alternate amino acid biosynthetic pathways in a preclinical model of pancreatic ductal adenocarcinoma. [Abstract]

2024 Jun 30;12(1):19. PMID: 38951899
Int J Mol Sci

Differential Oxygen Exposure Modulates Mesenchymal Stem Cell Metabolism and Proliferation through mTOR Signaling. [Abstract]

2022 Mar 29;23(7):3749. PMID: 35409106
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11:11:580407. PMID: 33343350
Chem Biol Interact

Hexavalent chromium promotes malignant transformation via enhanced translation of SUV39H1. [Abstract]

2026 Jan 25:424:111869. PMID: 41371533
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Transl Oncol

Enhanced efficacy of JAK1 inhibitor with mTORC1/C2 targeting in smoldering/chronic adult T cell leukemia. [Abstract]

2021 Jan;14(1):100913. PMID: 33129109
Cancers (Basel)

Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]

2022 Mar 19;14(6):1575. PMID: 35326726
iScience

Excipient of paclitaxel induces metabolic dysregulation and unfolded protein response. [Abstract]

2021 Sep 25;24(10):103170. PMID: 34646996
J Virol

Epstein-Barr virus-encoded latent membrane protein 2A promotes the epithelial-mesenchymal transition in nasopharyngeal carcinoma via metastatic tumor antigen 1 and mechanistic target of rapamycin signaling induction. [Abstract]

2014 Oct;88(20):11872-85. PMID: 25100829

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.

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.
J Photochem Photobiol B

Directly imaging the localisation and photosensitization properties of the pan-mTOR inhibitor, AZD2014, in living cancer cells. [Abstract]

2020 Dec:213:112055. PMID: 33142217
Microb Pathog

mTORC2-dependent autophagy inhibition regulates the replication of HSV-1 and adenovirus in viral keratitis & conjunctivitis. [Abstract]

2026 Apr:213:108349. PMID: 41628839
Immunol Cell Biol

Macrophage ERα promoted invasion of endometrial cancer cell by mTOR/KIF5B-mediated epithelial to mesenchymal transition. [Abstract]

2019 Jul;97(6):563-576. PMID: 30779215
Biochim Biophys Acta Gen Subj

Metabolic characterization of a paused-like pluripotent state. [Abstract]

2020 Aug;1864(8):129612. PMID: 32272203
J Surg Res

Anal Cancer Prevention Through the Topical Use of Single or Dual PI3K/mTOR Inhibitors. [Abstract]

2023 Feb:282:137-146. PMID: 36274448
bioRxiv

2026 May 2.
bioRxiv

2026 Mar 25.
bioRxiv

2026 Feb 4.
bioRxiv

Decreased tRNA abundance contributes to decreased translation elongation rate in a prolonged mitosis. [Abstract]

2026 Jan 14:2026.01.13.699274. PMID: 41648386
Res Sq

2025 Jul 18.
University of Washington

2025.
bioRxiv

Capacity for compensatory cyclin D2 response confers trametinib resistance in canine mucosal melanoma. [Abstract]

2025 Apr 26:2025.04.24.650512. PMID: 40568110
bioRxiv

2025 January 26.
Res Sq

Transcriptional Regulation of Protein Synthesis by Mediator Kinase Represents a Therapeutic Vulnerability in MYC-driven Medulloblastoma. [Abstract]

2024 Nov 1:rs.3.rs-5329081. PMID: 39574899
Res Sq

2024 Jul 15.
University of Washington

2024.
Free University of Berlin

2024.
bioRxiv

2024 May 15.
bioRxiv

Transcriptional Regulation of Protein Synthesis by Mediator Kinase in MYC-driven Medulloblastoma. [Abstract]

2024 Mar 13:2024.03.08.584103. PMID: 38559100
BioChem

2023 Nov 9, 3(4), 170-181.
bioRxiv

Protein interaction network analysis of mTOR signaling reveals modular organization. [Abstract]

2023 Aug 4:2023.08.04.552011. PMID: 37577705
bioRxiv

2023 May 30.
Patent

US20220054606A1.
Biomed Pharmacother

Combined inhibition of RNA polymerase I and mTORC1/2 synergize to combat oral squamous cell carcinoma. [Abstract]

2021 Jan:133:110906. PMID: 33190037

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (309 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Wei BR, et al. Efficacy, Tolerability, and Pharmacokinetics of Combined Targeted MEK and Dual mTORC1/2 Inhibition in a Preclinical Model of Mucosal Melanoma. Mol Cancer Ther. 2020 Nov;19(11):2308-2318.

[2]. Xu Z, et al. Sapanisertib attenuates pulmonary fibrosis by modulating Wnt5a/mTOR signalling. Basic & clinical pharmacology & toxicology. 2023 Sep;133(3):226-236.

[3]. Hussein AM, et al. Metabolic Control over mTOR-Dependent Diapause-like State. Developmental cell. 2020 Jan 27;52(2):236-250.e7. [Content Brief]

[4]. Zervantonakis IK, et al. Systems analysis of apoptotic priming in ovarian cancer identifies vulnerabilities and predictors of drug response. Nature communications. 2017 Aug 28;8(1):365.

[5]. Akça E S, et al. Inhibition of mTORC1/2 by INK-128 Impairs in vitro Oocyte Maturation in Mice[J]. Yeditepe Journal of Health Sciences, 2025, 3: 130-138.

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.

Complete Stock Solution Preparation Table

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.

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

Bioz

Sapanisertib

56 Cited Publications

100 mg Get Quote

Subscribe to the

MedChemExpress

Newsletter

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Sapanisertib

Publications Citing Use of MedChemExpress (MCE) Sapanisertib

All mTOR Isoforms

All Akt Isoforms

All ERK Isoforms

All CDK Isoforms

All Ribosomal S6 Kinase (RSK) Isoforms

All HIF/HIF Prolyl-Hydroxylase Isoforms

All Wnt Isoforms