1422006-47-0
Chemical Structure
Sapanisertib phosphate
Synonym(s): INK-128 phosphate; MLN0128 phosphate; TAK-228 phosphate
- CAS No.: 1422006-47-0
- Formula:C15H18N7O5P
- Molecular Weight:407.33
IUPAC Name: 5-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)benzo[d]oxazol-2-amine phosphate
InChIKey: ZCBRZSQEWLAEHT-UHFFFAOYSA-N
SMILES: O=P(O)(O)O.N=1C=NC2=C(C1N)C(=NN2C(C)C)C=3C=CC=4OC(=NC4C3)N
Biological Activity: 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[1][2][3][4][5].
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Sapanisertib phosphate | 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. | |||||||||||||||||||||
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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.
