product name INK 128 (MLN0128)
Description: INK 128 (also known as MLN0128) is a potent, orally bioavailable and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; it displayed >200-fold less potent to class I PI3K isoforms, and is superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). INK128 binds to and inhibits both TORC1 and TORC2 complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation.
References: Nature. 2012 Feb 22;485(7396):55-61; Drug Discov Today Ther Strateg. 2009; 6(2):47-55.
309.33
Formula
C15H15N7O
CAS No.
1224844-38-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 62 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (6.5 mM)
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 30mg/mL
Synonyms
MLN-0128; Sapanisertib
other peoduct :
| In Vitro |
Kinase Assay: Cell Assay: INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. 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. |
|---|---|
| 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. Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models. |
| Animal model | |
| Formulation & Dosage | |
| References | Nature. 2012 Feb 22;485(7396):55-61; Drug Discov Today Ther Strateg. 2009; 6(2):47-55. |
Integrin Antagonist 3 (hydrochloride)
