SPK-98

Molecule Name

SPK-98

 Id

 

Structure

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Molecular Formula

C28H22F3N5O

Molecular Weight

 .5132

Appearance

 

Purity

> 95%

 

DMSO, Methanol

 

SPK98 is a dual human mTOR and ATR inhibitor. It has been shown to exhibit a nanomolar range of enzyme inhibition through in vitro assays against ATR protein.  is a promising molecule that can be used against cancers with p53 or ATM deficiency.

Biological Activity

  1. Potent mTOR/ATR dual kinase inhibitor showing complete inhibition of p70 S6K at a concentration of 50 nM as well as complete inhibition of pChk1 Ser 317 at a concentration of 250 nM.
  2. Better t1/2 of 157 minutes in comparison with Torin 2.
  3. GI50 of 56.01 nM, 50.43 nM, 14.5 nM, 2.8 nM against HCT 116, HeLa, MCF7, MDAMB-231 cell lines respectively.
  4.  

Storage

20ºC for long term, 4ºC for short term use

References
1. Shaik, A., Bhakuni, R., & Kirubakaran, S. (2018). Design, synthesis, and docking studies of new Torin2 analogs as potential ATR/mTOR kinase inhibitors. Molecules, 23(5), 992.
2. Shaik, A., Bhakuni, R., & Kirubakaran, S. (2018). Design, synthesis, and docking studies of new Torin2 analogs as potential ATR/mTOR kinase inhibitors. Molecules, 23(5), 992.Bhakuni R. et al. Bioorganic & Medicinal Chemistry Letters, 2020, 30, 127517
3. Priya, B., Dubey, G., & Kirubakaran, S. (2023). Exploring SPK98 for the selective sensitization of ATM-or P53-deficient cancer cells. ACS omega, 8(5), 4954-4962.

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