INK 128 (MLN0128)

Catalog No.S2811

INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.

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INK 128 (MLN0128) Chemical Structure

INK 128 (MLN0128) Chemical Structure
Molecular Weight: 309.33

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INK 128 (MLN0128) is available in the following compound libraries:

mTOR Inhibitors with Unique Features

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Product Description

Biological Activity

Description INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
Targets mTOR [3]
(Cell-free assay)
mTOR [3]
(Cell-free assay)
PI3Kα [3]
(Cell-free assay)
PI3Kγ [3]
(Cell-free assay)

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IC50 1.4 nM(Ki) 1.4 nM(Ki) 219 nM 221 nM
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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
PANC-1 NWjRbpZ3S2WubDDWbYFjcWyrdImgRZN{[Xl?NGTucokyNTFyMDDuUS=>NEHUTpc4OiCqNV2z[lA{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?=NGjxdGUzPDl5MUW0OC=>
PANC-1 NV\HbW5oS2WubDDWbYFjcWyrdImgRZN{[Xl?MknJOVAhdk1?MVyyOE06PiCqMki5bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHlidHnt[UBl\XCnbnTlcpRtgQ>?MnfSNlQ6PzF3NES=
MIA PaCa-2NXHGc2F3S2WubDDWbYFjcWyrdImgRZN{[Xl?MmPlNU0yODBibl2=MmnWO|IhcA>?M{LrOIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?MnyxNlQ6PzF3NES=
PANC-1 NFq4[G1CeG:ydH;zbZMhSXO|YYm=M1qwRVExNTFyMDDuUS=>NHjvN|I4OiCqNYfQVm41cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=>NYjC[YJyOjR7N{G1OFQ>
PANC-1 M{fXV2Z2dmO2aX;uJGF{e2G7MmPhNVAwPTBibl2=MWWyOEBpMXHkdoFu[XSrY3HscJkhcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKDSHLVLQNU1UPktzIDjtWG9TSzFiYXP0bZZifGmxbjDpcoRq[2G2b4LzLUBidmRiQXv0JIF1KFOncjC0O|MhMHSqZTDtWG9TSzJiYXP0bZZifGmxbjDpcoRq[2G2b4KpNUDXb|lROjR7N{G1OFQ>
PANC-1 NGHVcGlHfW6ldHnvckBCe3OjeR?=NV3ITo43PTBibl2=NV7Lc2RiPDhiaB?=NUK1Tnhy\Gm|coXweJMh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?=NXvpXXFtOjR7N{G1OFQ>
PANC-1 M1zLdGZ2dmO2aX;uJGF{e2G7M13xNlExKG6PNIXKV284OiCqMXrpcoNz\WG|ZYOg[4Vu[2m2YXLpcoUhe2Wwc3n0bZZqfHl?NHXRfJozPDl5MUW0OC=>

... Click to View More Cell Line Experimental Data

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]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Liu A, et al. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55.

[2] Jessen K, et al. Mol Cancer Ther. 2009, 8(12), Meeting Abstract Supplement.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02575339 Recruiting Hepatocellular Carcinoma|Liver Cancer|HCC Bert ONeil, MD|Hoosier Cancer Research Network|Millennium  ...more Bert ONeil, MD|Hoosier Cancer Research Network|Millennium Pharmaceuticals, Inc.|Big Ten Cancer Research Consortium July 2016 Phase 1|Phase 2
NCT02756364 Not yet recruiting Breast Neoplasms Millennium Pharmaceuticals, Inc. June 2016 Phase 2
NCT02725268 Recruiting Endometrial Neoplasms Millennium Pharmaceuticals, Inc.|European Network of Tran  ...more Millennium Pharmaceuticals, Inc.|European Network of Translational Research in Ovarian Cancer - EUTROC|European Network of Individualized Treatment in Endometrial Cancer - ENITEC June 2016 Phase 2
NCT02724020 Recruiting Clear-cell Metastatic Renal Cell Carcinoma Millennium Pharmaceuticals, Inc. June 2016 Phase 2
NCT02719691 Recruiting Metastatic Breast Cancer|Solid Tumors University of Colorado, Denver May 2016 Phase 1

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Chemical Information

Download INK 128 (MLN0128) SDF
Molecular Weight (MW) 309.33
Formula

C15H15N7O

CAS No. 1224844-38-5
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 62 mg/mL (200.43 mM)
Ethanol 2 mg/mL (6.46 mM)
Water <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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