Sapanisertib (MLN0128)

Catalog No.S2811 Batch:S281103

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Technical Data

Formula

C15H15N7O
Molecular Weight 309.33 CAS No. 1224844-38-5
Solubility (25°C)* In vitro DMSO 62 mg/mL (200.43 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Sapanisertib (MLN0128, INK 128, TAK-228) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
Targets
mTOR [3]
(Cell-free assay)		 mTOR [3]
(Cell-free assay)		 PI3Kα [3]
(Cell-free assay)		 PI3Kγ [3]
(Cell-free assay)		 PI3Kδ [3]
(Cell-free assay)		 View More
1.4 nM(Ki) 1.4 nM(Ki) 219 nM 221 nM 230 nM
In vitro

INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. [1]

As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors. [2]
In vivo

In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day. [1]

Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models. [2]

Protocol (from reference)

Animal Study:

[3]
  • Animal Models

    Nude mice

  • Dosages

    0.3 and 1 mg/kg

  • Administration

    o.g.

Customer Product Validation

Data from [Data independently produced by Biochem Biophys Res Commun, 2013, 440(4), 701-6]

, , Antonino Maria Spart from University of Bologn

,

Data from [Data independently produced by , , Hepatology, 2017, 66(6):1920-1933]

Selleck's Sapanisertib (MLN0128) has been cited by 134 publications

PI3K/mTOR inhibition induces tumour microenvironment remodelling and sensitises pS6high uterine leiomyosarcoma to PD-1 blockade [ Clin Transl Med, 2024, 14(5):e1655] PubMed: 38711203
PI3K/mTOR inhibition induces tumour microenvironment remodelling and sensitises pS6high uterine leiomyosarcoma to PD-1 blockade [ Clin Transl Med, 2024, 14(5):e1655] PubMed: 38711203
Starvation-induced phosphorylation activates gasdermin A to initiate pyroptosis [ Cell Rep, 2024, 43(9):114728] PubMed: 39264808
Different Impacts of DNA-PK and mTOR Kinase Inhibitors in Combination with Ionizing Radiation on HNSCC and Normal Tissue Cells [ Cells, 2024, 13(4)304] PubMed: 38391917
Epstein-Barr Virus Latent Membrane Protein 2A (LMP2A) Enhances ATP Production in B Cell Tumors through mTOR and HIF-1α [ Int J Mol Sci, 2024, 25(7)3944] PubMed: 38612754
The highly selective and oral phosphoinositide 3-kinase delta (PI3K-δ) inhibitor roginolisib induces apoptosis in mesothelioma cells and increases immune effector cell composition [ Transl Oncol, 2024, 43:101857] PubMed: 38412661
Preclinical evaluation of the third-generation, bi-steric mechanistic target of rapamycin complex 1-selective inhibitor RMC-6272 in NF2-deficient models [ Neurooncol Adv, 2024, 6(1):vdae024] PubMed: 38476930
Evolutionarily divergent mTOR remodels translatome for tissue regeneration [ Nature, 2023, 620(7972):163-171] PubMed: 37495694
Histopathologic and proteogenomic heterogeneity reveals features of clear cell renal cell carcinoma aggressiveness [ Cancer Cell, 2023, 41(1):139-163.e17] PubMed: 36563681
mTOR inhibition reprograms cellular proteostasis by regulating eIF3D-mediated selective mRNA translation and promotes cell phenotype switching [ Cell Rep, 2023, 42(8):112868] PubMed: 37494188

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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