INK 128 (MLN0128)

INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM; >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

Validation & Quality Control

Customer Reviews(2)

Quality Control & MSDS

Related Compound Libraries

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

mTOR Inhibitors with Unique Features

Product Information

  • Inhibition Profile
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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM; >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 [1] mTOR [3] PI3Kα [3] PI3Kγ [3] PI3Kδ [3] PI3Kβ [3]
IC50 1 nM 1.4 nM(Ki) 219 nM 221 nM 230 nM 5293 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]
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

Protocol(Only for Reference)

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
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 2014-08-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02197572 Not yet recruiting Advanced Solid Tumors Millennium Pharmaceuticals, Inc. July 2014 Phase 1
NCT02159989 Recruiting Gastrinoma|Glucagonoma|Insulinoma|Pancreatic Polypeptide Tumor|Recurrent Islet Cell Carcinoma|Recurrent Ovarian Epithelial Cancer|Recurrent Ovarian  ...more Gastrinoma|Glucagonoma|Insulinoma|Pancreatic Polypeptide Tumor|Recurrent Islet Cell Carcinoma|Recurrent Ovarian Epithelial Cancer|Recurrent Ovarian Germ Cell Tumor|Somatostatinoma|Stage IIIA Ovarian Epithelial Cancer|Stage IIIA Ovarian Germ Cell Tumor|Stage IIIB Ovarian Epithelial Cancer|Stage IIIB Ovarian Germ Cell Tumor|Stage IIIC Ovarian Epithelial Cancer|Stage IIIC Ovarian Germ Cell Tumor|Stage IV Ovarian Epithelial Cancer|Stage IV Ovarian Germ Cell Tumor|Unspecified Adult Solid Tumor, Protocol Specific National Cancer Institute (NCI) June 2014 Phase 1
NCT02142803 Recruiting Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Endometrial Clear Cell Carcinoma|Endometrial Papillary Serous Carcinoma|Ovarian  ...more Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Endometrial Clear Cell Carcinoma|Endometrial Papillary Serous Carcinoma|Ovarian Clear Cell Cystadenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Cystadenocarcinoma|Ovarian Serous Cystadenocarcinoma|Recurrent Adult Brain Tumor|Recurrent Endometrial Carcinoma|Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Primary Peritoneal Cavity Cancer|Stage IIIA Fallopian Tube Cancer|Stage IIIA Ovarian Epithelial Cancer|Stage IIIA Primary Peritoneal Cavity Cancer|Stage IIIB Fallopian Tube Cancer|Stage IIIB Ovarian Epithelial Cancer|Stage IIIB Primary Peritoneal Cavity Cancer|Stage IIIC Fallopian Tube Cancer|Stage IIIC Ovarian Epithelial Cancer|Stage IIIC Primary Peritoneal Cavity Cancer|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Epithelial Cancer|Stage IV Primary Peritoneal Cavity Cancer|Unspecified Adult Solid Tumor, Protocol Specific National Cancer Institute (NCI) May 2014 Phase 1
NCT02133183 Recruiting Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor National Cancer Institute (NCI) May 2014 --
NCT02091531 Recruiting Metastatic Castration-Resistant Prostate Cancer Memorial Sloan-Kettering Cancer Center|Millennium Pharmaceuticals, Inc. March 2014 Phase 2

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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 DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 62 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol 2 mg/mL (6 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

Research Area

Customer Reviews (2)


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Rating
Source Antonino Maria Spartà from University of Bologna. 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

Product Citations (2)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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