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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

INK-128

HY-13328

(Sapanisertib; MLN0128)

INK-128

INK-128 Chemical Structure

INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms.

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Product name: INK-128
Cat. No.: HY-13328

INK-128 Data Sheet

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    Purity: 99.55%

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Related Compound Libraries

Biological Activity of INK-128

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 [1]
Target: mTOR
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].

Chemical Information

M.Wt 309.33 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C₁₅H₁₅N₇O
CAS No 1224844-38-5
Solvent & Solubility

10 mM in DMSO

Preparing Stock Solutions

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

Clinical Information of INK-128

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

References on INK-128

Inhibitor Kit

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