|
Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
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.) |
||||
Preparing Stock Solutions
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 |
|
|||||||||||
| 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: |
|
|---|
References
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 127 publications
| 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 |
| 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 |
| Activation of GPR44 decreases severity of myeloid leukemia via specific targeting of leukemia initiating stem cells [ Cell Rep, 2023, 42(7):112794] | PubMed: 37459233 |
| BMAL1/p53 mediating bronchial epithelial cell autophagy contributes to PM2.5-aggravated asthma [ Cell Commun Signal, 2023, 21(1):39] | PubMed: 36803515 |
| A drug-resistant mutation in plant target of rapamycin validates the specificity of ATP-competitive TOR inhibitors in vivo [ Plant J, 2023, 10.1111/tpj.16564] | PubMed: 38011587 |
| Identification and subsequent validation of transcriptomic signature associated with metabolic status in endometrial cancer [ Sci Rep, 2023, 13(1):13763] | PubMed: 37612452 |
| Androgen receptor-dependent regulation of metabolism in high grade bladder cancer cells [ Sci Rep, 2023, 13(1):1762] | PubMed: 36720985 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.