SBP-7455 free base · Synonyms: SBP 7455 · SBP7455

SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor.

For research use only. Not for human or veterinary use.

Target ULK Autophagy

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

SBP-7455 structure

CAS No.: 1884222-74-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 g	USD 820.00	BP-01945-1g	In stock	Get quote
5 g	Inquire	BP-01945-5g	Inquire	Inquire
10 g	Inquire	BP-01945-10g	Inquire	Inquire

Need another size or custom synthesis? Request a quote.

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.

Biological activity

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.

Identifiers

SMILES: FC(F)(F)C1=CN=C(N=C1NC2CC2)NC3=CC=C(C(OC)=C3)OC
InChIKey: BQROJYIEHOOQBY-UHFFFAOYSA-N

Specifications

MW (average): 354.3270
Formula: C₁₆H₁₇F₃N₄O₂
CAS No.: 1884222-74-5
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 125 mg/mL

Documents

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

Same target

Search ULK

Same research area

Search Cancer