Description
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.
Product information
CAS Number: 1884222-74-5
Molecular Weight: 354.33
Formula: C16H17F3N4O2
Chemical Name: N4-cyclopropyl-N2-(3,4-dimethoxyphenyl)-5-(trifluoromethyl)pyrimidine-2,4-diamine
Smiles: COC1=CC=C(C=C1OC)NC1=NC(NC2CC2)=C(C=N1)C(F)(F)F
InChiKey: BQROJYIEHOOQBY-UHFFFAOYSA-N
InChi: InChI=1S/C16H17F3N4O2/c1-24-12-6-5-10(7-13(12)25-2)22-15-20-8-11(16(17,18)19)14(23-15)21-9-3-4-9/h5-9H,3-4H2,1-2H3,(H2,20,21,22,23)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (352.78 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
SBP-7455 (compound 26; 72 h) treatment inhibits cell growth with an IC50 of 0.3 μM for MDA-MB-468 cells. SBP-7455 inhibits starvation-induced autophagic flux in TNBC cells that are dependent on autophagy for survival.
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. 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.
Products are for research use only. Not for human use.
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