4-[(3R)-3-methylmorpholin-4-yl]-6-[(2R)-2-(trifluoro
methyl)piperidin-1-yl]-1,2-dihydropyridin-2-one manufacturers
- SB02024
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- $2380.00
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2026-07-27
- CAS:2126737-28-6
- Purity:
- Supply Ability: 10g
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| | 4-[(3R)-3-methylmorpholin-4-yl]-6-[(2R)-2-(trifluoro
methyl)piperidin-1-yl]-1,2-dihydropyridin-2-one Basic information |
| | 4-[(3R)-3-methylmorpholin-4-yl]-6-[(2R)-2-(trifluoro
methyl)piperidin-1-yl]-1,2-dihydropyridin-2-one 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 |
| | 4-[(3R)-3-methylmorpholin-4-yl]-6-[(2R)-2-(trifluoro
methyl)piperidin-1-yl]-1,2-dihydropyridin-2-one Usage And Synthesis |
| 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.
[4] MATHEUS DYCZYNSKI . Targeting autophagy by small molecule inhibitors of vacuolar protein sorting 34 (Vps34) improves the sensitivity of breast cancer cells to Sunitinib[J]. Cancer letters, 2018, 435: Pages 32-43. DOI: 10.1016/j.canlet.2018.07.028 |
| | 4-[(3R)-3-methylmorpholin-4-yl]-6-[(2R)-2-(trifluoro
methyl)piperidin-1-yl]-1,2-dihydropyridin-2-one Preparation Products And Raw materials |
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