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SB02024

Chemical Structure : SB02024

CAS No.: 2126737-28-6

SB02024 (SB-02024)

Catalog No.: PC-35505Not For Human Use, Lab Use Only.

SB02024 is a novel highly potent, selective, ATP competitive, orally active inhibitor of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times selective towards other PI3K isoenzymes.

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Biological Activity

SB02024 (SB 02024) is a novel highly potent, selective, ATP competitive, orally active inhibitor of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times selective towards other PI3K isoenzymes.
SB02024 is also highly selective at 1 uM in the DiscoveRx ScanMax panel of 468 kinases.
SB02024 reduces the number of GFP-2xFYVE puncta with IC50 of 14 nM, induces a dose-dependent increase in levels of NCOA4 and p62.
SB02024 blocks autophagy in vitro and reduces xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7.
SB02024 also significantly potentiates cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro.

Physicochemical Properties

M.Wt 345.37
Formula C16H22F3N3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((R)-3-methylmorpholino)-6-((R)-2-(trifluoromethyl)piperidin-1-yl)pyridin-2(1H)-one

References

1. Dyczynski M, et al. Cancer Lett. 2018 Jul 25. pii: S0304-3835(18)30486-5.

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