ChemicalBook CAS DataBase List 2126737-28-6

2126737-28-6

Name	4-[(3R)-3-methylmorpholin-4-yl]-6-[(2R)-2-(trifluoro methyl)piperidin-1-yl]-1,2-dihydropyridin-2-one
CAS	2126737-28-6
Molecular Formula	C16H22F3N3O2
MDL Number	MFCD32853054
Molecular Weight	345.36
MOL File	2126737-28-6.mol

Chemical Properties

Boiling point	432.2±45.0 °C(Predicted)
density	1.288±0.06 g/cm3(Predicted)
solubility	Acetonitrile: Slightly soluble: 0.1-1 mg/ml DMSO: Sparingly soluble: 1-10 mg/ml
form	Solid
pka	10.99±0.10(Predicted)
color	White to off-white

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P264-P270-P301+P312-P330-P501-P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P

Hazard Information

Description

SB02024 is a VPS34 inhibitor. SB02024 activates cGAS-STING signaling and sensitizes tumors to STING agonist. SB02024 blocked autophagy in vitro and reduced xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7, in vivo. Vps34 inhibitor significantly potentiated cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro in monolayer cultures and when grown as multicellular spheroids. Our data suggests that inhibition of autophagy significantly improves sensitivity to Sunitinib and Erlotinib and that Vps34 is a promising therapeutic target for combination strategies in breast cancer.

Uses

SB02024 is a potent and orally active VPS34 inhibitor. SB02024 inhibits Vps34 kinase activity. SB02024 induces CCL5 and CXCL10 via STAT1/IRF7. SB02024 shows anticancer activity[1][2][3].

in vivo

SB02024 (20 mg/kg, Oral gavage) decreases the tumor growth and improves the effect benefit of anti-PD-L1/PD-1^[1].
SB02024 increases the levels of CCL5 and CXCL10 in the blood plasma of B16-F10 and CT26 tumor-bearing mice, but dose not increase CCL5 or CXCL10 levels in the blood of non-tumor-bearing mice^[1].

Animal Model:	C57BL/6, BALB/C, immunodeficient NSG mice (7 weeks old)^[1]
Dosage:	20 mg/kg
Administration:	Oral gavage
Result:	Decreased the tumor growth and weight of B16-F10 and CT26 and prolonged the survival of tumor-bearing mice.

IC 50

Vps34; STAT1

References

[1] Noman MZ, et al. Inhibition of Vps34 reprograms cold into hot inflamed tumors and improves anti-PD-1/PD-L1 immunotherapy. Sci Adv. 2020 Apr 29;6(18):eaax7881. DOI:10.1126/sciadv.aax7881
[2] Yu Y, et al. Combining VPS34 inhibitors with STING agonists enhances type I interferon signaling and anti-tumor efficacy. Mol Oncol. 2024 Mar 20. DOI:10.1002/1878-0261.13619
[3] Bassam Claude JANJI, et al. Biomarker. Patent WO2020008046 A1.

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