Cat. No.: HY-13328A

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Sapanisertib phosphate

Name: Sapanisertib phosphate
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SKU: HY-13328A
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(Synonyms: INK-128 phosphate; MLN0128 phosphate; TAK-228 phosphate)

59 Cited Publications

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Based on 59 publication(s) in Google Scholar

Sapanisertib (INK-128; MLN0128; TAK-228) phosphate is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib phosphate 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 phosphate is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.

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

CAS No.: 1422006-47-0
Formula: C₁₅H₁₈N₇O₅P
Molecular Weight:407.33

Storage:

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

Sapanisertib phosphate Chemical Structure

CAS No.: 1422006-47-0

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Top Publications Citing

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (59)
Purity & Documentation
References
Calculators
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 :

In Vitro

Carbohydrate MetabolismCell Cycle RegulationAnti-cancerApoptosisOthers

Carbohydrate Metabolism

Sapanisertib (INK-128) (200 nM; overnight) phosphate enhances glycolytic capacity and alters lipid metabolism in mESCs^[3].

Cell Cycle Regulation

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].

Anti-cancer

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].

Anti-cancer

Apoptosis

Sapanisertib (10 nM; 24 h) phosphate induces apoptosis in M1 and M5 canine melanoma cell lines^[1].

Anti-cancer

Cell Cycle Regulation

Apoptosis

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].

Others

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.

Parmacokinetics

Species	Dose	Route	C_max	T_1/2	AUC
Mice^[1]	2.0 mg/kg	p.o.	215 ng/mL	12 h	931 ng·h/mL

In Vivo

Anti-cancerOthers

Anti-cancer

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].

Others

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.

Related Protocols :

Chemical Information

CAS No. 1422006-47-0
Molecular Weight 407.33
Formula C₁₅H₁₈N₇O₅P
SMILES

O=P(O)(O)O.N=1C=NC2=C(C1N)C(=NN2C(C)C)C=3C=CC=4OC(=NC4C3)N
Synonyms

INK-128 phosphate; MLN0128 phosphate; TAK-228 phosphate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (59)

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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

2026 Sep 11.
Nat Commun

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

2017 Jun 8:8:15617. PMID: 28593995

Sapanisertib phosphate 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 phosphate 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 phosphate 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 phosphate 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 Sep 13.
Friedrich Schiller University Jena

2026.
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
University of Washington

2025.
Res Sq

2025 Jul 18.
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

Purity & Documentation

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.

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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.

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Sapanisertib phosphate

59 Cited Publications

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Sapanisertib phosphate

Publications Citing Use of MedChemExpress (MCE) Sapanisertib phosphate

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