INK 128 (MLN0128) 化学構造
分子量: 309.33

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Quality Control & MSDS

製品説明

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    mTOR製品生物活性の比較
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    併用療法

製品の説明

生物活性

製品説明 INK 128 (MLN0128)は、有力で選択的なmTOR 阻害剤で、 IC50 が 1 nMです。
ターゲット mTOR
IC50 1 nM [1]
In vitro試験 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  MXTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXOxMVExOCCwTR?= NFjmdXE4OiCq NF\2e25qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MYSyOFk4OTV2NB?=
PANC-1  NHThWJJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MX:1NEBvVQ>? MViyOE06PiCq MVHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSC2aX3lJIRmeGWwZHXueIx6 M4nRNVI1QTdzNUS0
MIA PaCa-2 M4\MTmNmdGxiVnnhZoltcXS7IFHzd4F6 NFfIS4MyNTFyMDDuUS=> MWi3NkBp M{D4UYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MYqyOFk4OTV2NB?=
PANC-1  M{TkOWFxd3C2b4Ppd{BCe3OjeR?= MX6xNE0yODBibl2= MkPSO|IhcA>? M2jjPYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NE[y[4IzPDl5MUW0OC=>
PANC-1  Mor4SpVv[3Srb36gRZN{[Xl? NYXndopEOTBxNUCgcm0> MljlNlQhcA>? NEf5dItlemGvYYTpZ4FtdHliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIETFMWJROS2VNluxJEhuXE:UQ{GgZYN1cX[jdHnvckBqdmSrY3H0c5J{MSCjbnSgRYt1KGG2IGPldkA1PzNiKITo[UBuXE:UQ{KgZYN1cX[jdHnvckBqdmSrY3H0c5Iq MYWyOFk4OTV2NB?=
PANC-1  MmDVSpVv[3Srb36gRZN{[Xl? NWLG[JJGPTBibl2= MV20PEBp NHjpemhlcXO{dYD0d{Bk\WyuIHP5Z4xmKHC{b3fy[ZN{cW:w NFzEeXYzPDl5MUW0OC=>
PANC-1  NHrTTXJHfW6ldHnvckBCe3OjeR?= MYqxNEBvVQ>? NFn2eVk4OiCq NF3J[JdqdmO{ZXHz[ZMh\2WvY3n0ZYJqdmVic3Xud4l1cX[rdIm= NH:zbVczPDl5MUW0OC=>

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 INK 128 is currently in Phase I clinical trials in patients with relapsed or refractory multiple myeloma or waldenstrom macroglobulinemia.
特集

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

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
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

参考

化学情報

Download INK 128 (MLN0128) SDF
分子量 309.33
化学式

C15H15N7O

CAS No. 1224844-38-5
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 62 mg/mL (200.43 mM)
エタノール 2 mg/mL (6.46 mM)
<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.
化学名 3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine

カスタマーフィードバック (3)


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Rating
Source Biochem Biophys Res Commun, 2013, 440(4), 701-6. INK 128 (MLN0128) purchased from Selleck
Method CCK-8 cell viability assay
Cell Lines Hep-2, SCC-9 cells
Concentrations 0.1 uM
Incubation Time 72 h
Results It found that AZD8055 was more potent than mTORC1 inhibitor rapamycin and Akt/mTOR dual inhibitor LY 294002 in killing of Hep-2 (D) and SCC-9 (E) cells. AZD2014 and INK-128, two other mTORC1/mTORC2 dual inhibitors, were also shown to inhibit the survival of Hep-2 and SCC-9 cells (D and E).

Click to enlarge
Rating
Source Antonino Maria Spart from University of Bologn. INK 128 (MLN0128) purchased from Selleck
Method Western Blot/MTT
Cell Lines Molt-4 leukemia cell
Concentrations 1.9 μM
Incubation Time 48 h
Results PI3K Inhibitor INK-128 was able to block Molt-4 leukemia cell line proliferation after 48 h with a measured IC50 of around 1.9 mM. Apoptosis induction assessed by western blot, demonstrated a limited cleavage of Caspase 7.

Click to enlarge
Rating
Source INK 128 (MLN0128) purchased from Selleck
Method ELISA
Cell Lines Bone marrow derived macrophages
Concentrations 1 nM
Incubation Time 1 h
Results

文献中の引用 (7)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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