Cas No.: | 2126737-28-6 |
Chemical Name: | SB02024 |
Synonyms: | SB02024;SB-02024;SB 02024 |
SMILES: | O=C1NC(N2[C@@H](C(F)(F)F)CCCC2)=CC(N3[C@H](C)COCC3)=C1 |
Formula: | C16H22F3N3O2 |
M.Wt: | 345.36 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | 1. Dyczynski M, et al. Cancer Lett. 2018 Jul 25. pii: S0304-3835(18)30486-5. |
Description: | 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; SB02024 is also highly selective at 1 uM in the DiscoveRx ScanMax panel of 468 kinases; reduces the number of GFP-2xFYVE puncta with IC50 of 14 nM, induces a dose-dependent increase in levels of NCOA4 and p62; blocks autophagy in vitro and reduces xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7; also significantly potentiates cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro. |
Target: | Vps34 1 nM |
References: | 1. Dyczynski M, et al. Cancer Lett. 2018 Jul 25. pii: S0304-3835(18)30486-5. |