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INK128

Cat. No. M2151
INK128 Structure
Synonym:

MLN0128

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 110 In stock
50mg USD 280 In stock
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Quality Control
Biological Activity

INK128 (also known as MLN0128) is also an orally bioavailable mTOR inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity. INK128 blocks the phosphorylation of downstream substrates of both TORC1 and TORC2. INK128 (MLN0128) exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. INK128 interferes with the growth of cell lines which are resistant to rapamycin and pan-PI3K inhibitors. Oral administration of INK128 (MLN0128) inhibits angiogenesis and tumor growth in several xenograft models. In vitro and in vivo studies showed that p-4EBP1 and p-Akt inhibition could be predictive markers of TORC2 inhibition in MM cell lines. Dual TORC1/2 inhibition showed better inhibition of adhesion to BM microenvironmental cells and inhibition of homing in vivo.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 309.33
Formula C15H15N7O
CAS Number 1224844-38-5
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Cancer Biology & Therapy (2015). Figure 1. INK-128
Method MTT assay
Cell Lines HT-29 cells
Concentrations 5, 25 and 100 nM
Incubation Time 72 h
Results INK-128 dose-dependently inhibited the number of survival colonies, while increasing the PtdIns staining in HT-29 cells.
Rating
References

Defining the role of TORC1/2 in multiple myeloma.
Maiso P, et al. Blood. 2011 Dec 22;118(26):6860-70. PMID: 22045983.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: INK128, MLN0128 supplier, mTOR, inhibitors

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