For research use only. Not for therapeutic Use.
INK-128 (also known as Sapanisertib)（Cat No.:I000862）is a potent, selective inhibitor of the mechanistic target of rapamycin (mTOR), specifically targeting both mTORC1 and mTORC2 complexes. By inhibiting mTOR signaling, INK-128 disrupts pathways involved in cancer cell growth, proliferation, and survival, making it a promising candidate in oncology. It has shown efficacy in preclinical studies for a variety of cancers, including solid tumors and hematologic malignancies. INK-128 is particularly valuable in overcoming resistance to first-generation mTOR inhibitors, offering potential in cancer therapies targeting hyperactive mTOR signaling pathways.
| Catalog Number | I000862 |
| CAS Number | 1224844-38-5 |
| Synonyms | 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine |
| Molecular Formula | C₁₅H₁₅N₇O |
| Purity | ≥95% |
| Target | mTOR |
| Solubility | DMSO 62 mg/ml; Water <1 mg/ml |
| Storage | 3 years -20℃ powder |
| IC50 | 1 nM [1] |
| IUPAC Name | 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine |
| InChI | InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19) |
| InChIKey | GYLDXIAOMVERTK-UHFFFAOYSA-N |
| SMILES | CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N |
| Reference | </br>1:Dual mTORC1/2 inhibition by INK-128 results in antitumor activity in preclinical models of osteosarcoma. Jiang H, Zeng Z.Biochem Biophys Res Commun. 2015 Dec 4-11;468(1-2):255-61. doi: 10.1016/j.bbrc.2015.10.119. Epub 2015 Oct 26. PMID: 26514724 </br>2:Dual targeting of mTORC1 and mTORC2 by INK-128 potently inhibits human prostate cancer cell growth in vitro and in vivo. Jiang SJ, Wang S.Tumour Biol. 2015 Sep;36(10):8177-84. doi: 10.1007/s13277-015-3536-6. Epub 2015 May 21. PMID: 25990456 </br>3:The preclinical evaluation of the dual mTORC1/2 inhibitor INK-128 as a potential anti-colorectal cancer agent. Li C, Cui JF, Chen MB, Liu CY, Liu F, Zhang QD, Zou J, Lu PH.Cancer Biol Ther. 2015;16(1):34-42. doi: 10.4161/15384047.2014.972274. PMID: 25692620 Free PMC Article</br>4:The novel mTORC1/2 dual inhibitor INK-128 suppresses survival and proliferation of primary and transformed human pancreatic cancer cells. Lou HZ, Weng XC, Pan HM, Pan Q, Sun P, Liu LL, Chen B.Biochem Biophys Res Commun. 2014 Jul 25;450(2):973-8. doi: 10.1016/j.bbrc.2014.06.081. Epub 2014 Jun 24. PMID: 24971544 |
