| Identification | Back Directory | [Name]
2,4-Pyrimidinediamine, N4-cyclopropyl-N2-(3,4-dimethoxyphenyl)-5-(trifluoromethyl)- | [CAS]
1884222-74-5 | [Synonyms]
sbp-7455
2,4-Pyrimidinediamine, N4-cyclopropyl-N2-(3,4-dimethoxyphenyl)-5-(trifluoromethyl)-
SBP-7455,ULK,TNBC,ULK2,ULK1,Unc-51 like kinase,sbp7455,Ser318,sbp 7455,Inhibitor,inhibit,Autophagy,pATG13,oral | [Molecular Formula]
C16H17F3N4O2 | [MDL Number]
MFCD32899898 | [MOL File]
1884222-74-5.mol | [Molecular Weight]
354.33 |
| Chemical Properties | Back Directory | [Boiling point ]
490.2±55.0 °C(Predicted) | [density ]
1.405±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml,Ethanol: 1 mg/ml | [form ]
A crystalline solid | [pka]
3.29±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research[1]. | [in vivo]
A single dose of SBP-7455 (compound 26) (30 mg/kg) is orally administered to mice. The Tmax for SBP-7455 is approximately 1 h,? the Cmax is 990 nM and the T1/2 is 1.7 h. The plasma concentration of SBP-7455 remains above the ULK1 IC50 for almost 4 h after oral dosing[1].
?
The mice are dosed with SBP-7455 (compound 26) (10 mg/kg) by oral gavage, and liver samples were collected after 2 h. The results reveals robust inhibition of pATG13 (Ser318), as well as downregulation of total ATG13 and ULK1 levels by SBP-7455[1]. | [IC 50]
ULK1: 13 nM (IC50); ULK2: 476 nM (IC50) | [References]
[1] Huiyu Ren, et al. Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer. J Med Chem. 2020 Dec 10;63(23):1460 DOI:10.1021/acs.jmedchem.0c00873 |
|
| Company Name: |
DC Chemicals
|
| Tel: |
021-58447131 13564518121 |
| Website: |
www.chemicalbook.com/showsupplierproductslist927327/0.htm |
| Company Name: |
ChemeGen 中国
|
| Tel: |
18818260767 |
| Website: |
https://www.chemegen.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|