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INK 128 (MLN0128)
MTOR(TORC-1/-2) inhibitor,potent and selective

INK 128 (MLN0128)

Catalog No. A8551
Size Price Stock Qty
5mg $80.00 In stock
10mg $100.00 In stock
50mg $250.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1.Heredia, Alonso, et al. "Targeting of mTOR catalytic site inhibits multiple steps of the HIV-1 lifecycle and suppresses HIV-1 viremia in humanized mice." Proceedings of the National Academy of Sciences (2015): 201511144. PMID:26170311

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Chemical structure

INK 128 (MLN0128)

Related Biological Data

INK 128 (MLN0128)

Related Biological Data

INK 128 (MLN0128)

Biological Activity

Description INK 128 (MLN0128) is a potent and selective inhibitor of mTOR with an IC50 value of 1 nM.
Targets mTOR PI3Kα PI3Kγ PI3Kδ PI3Kβ  
IC50 1 nM (Ki=1.4 nM) 219 nM 221 nM 230 nM 5293 nM  

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Chemical Properties

Cas No. 1224844-38-5 SDF Download SDF
Synonyms INK128; INK-128
Chemical Name 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine
Canonical SMILES CC(C)N1C2=C(C(=N1)C3=CC4=C(C=C3)OC(=N4)N)C(=NC=N2)N
Formula C15H15N7O M.Wt 309.33
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

INK 128 (MLN0128) is a selective inhibitor of mTOR with IC50 value of 1 nM [3].

mTOR (mammalian target of rapamycin) is an evolutionarily conserved serine/threonine kinase which combined PI3K/AKT/mTOR pathway and plays an important role in regulating many fundamental features of cell growth and division [1].

INK 128 (MLN0128) is a potent mTOR inhibitor. When tested with human pancreatic cancer cells, INK-128 treatment inhibited cell growth and survival via inhibiting mTOR in a time- and concentration- dependent manner [2]. In HER2-positive breast cell lines, INK 128 treatment significantly delayed cell cycle and inhibited cell proliferation through inhibiting mTOR [1].

In a ZR-75-1 breast cancer xenograft model, INK128 treatment in a dose of 0.3mg/Kg/day significantly inhibited tumor growth. When combined with other standard targeted therapy or chemotherapy such as sorafenib, sutent and paclitaxel, enhanced anti-tumor growth activity was observed. INK128 is reported to have excellent physiochemical properties and is currently undergoing preclinical evaluation [3]. When tested with MDA-MB361 mouse model, administration of INK 128 showed a resistance after 20 days, and combined with lapatinib resulted in long-lasting tumor regression [1].

References:
[1].  Garcia-Garcia, C., et al., Dual mTORC1/2 and HER2 blockade results in antitumor activity in preclinical models of breast cancer resistant to anti-HER2 therapy. Clin Cancer Res, 2012. 18(9): p. 2603-12.
[2].  Lou, H.Z., et al., The novel mTORC1/2 dual inhibitor INK-128 suppresses survival and proliferation of primary and transformed human pancreatic cancer cells. Biochem Biophys Res Commun, 2014. 450(2): p. 973-8.
[3].  Jessen K, et al. INK128 is a potent and selective TORC1/2 inhibitor with broad oral anti-tumor activity. AACR 2009 Molecular targets and cancer therapeutics meeting poster; Boston: 2009.