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INK-128 Chemical Structure
|Product name: INK-128|
|Cat. No.: HY-13328|
INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms.
IC50 value: 1 nM 
in vitro: 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 .
|M.Wt||309.33||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO 62 mg/ml; Water <1 mg/ml
|1 mg||5 mg||10 mg|
|1 mM||3.2328 mL||16.1640 mL||32.3279 mL|
|5 mM||0.6466 mL||3.2328 mL||6.4656 mL|
|10 mM||0.3233 mL||1.6164 mL||3.2328 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|INK-128||Millennium Pharmaceuticals Inc||Non-Hodgkin lymphoma||30-NOV-10||31-JAN-14||Phase 1||05-AUG-13|
|Millennium Pharmaceuticals Inc||Macroglobulinemia||30-NOV-10||31-JAN-14||Phase 1||05-AUG-13|
|Millennium Pharmaceuticals Inc||Advanced solid tumor||31-JUL-13||30-NOV-16||Phase 1||12-SEP-13|
|Millennium Pharmaceuticals Inc||Advanced solid tumor||31-JAN-10||31-MAR-15||Phase 1||25-JUL-13|
|Millennium Pharmaceuticals Inc||Advanced solid tumor||31-MAR-11||28-FEB-14||Phase 1||20-NOV-13|
|Millennium Pharmaceuticals Inc||Multiple myeloma||30-NOV-10||31-JAN-14||Phase 1||05-AUG-13|
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