A-1331852 free base · Synonyms: A 1331852 · A1331852

A-1331852 is a potent BCL-XL-selective inhibitor.

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

Target Bcl-2 Family

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

A-1331852 structure

CAS No.: 1430844-80-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 370.00	BP-02320-50mg	In stock	Get quote
100 mg	USD 592.00	BP-02320-100mg	In stock	Get quote
250 mg	USD 1,184.00	BP-02320-250mg	In stock	Get quote
500 mg	USD 1,890.00	BP-02320-500mg	In stock	Get quote
1 g	USD 3,030.00	BP-02320-1g	In stock	Get quote
2 g	USD 4,850.00	BP-02320-2g	In stock	Get quote
3 g	Inquire	BP-02320-3g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

A-1331852 is a potent BCL-XL-selective inhibitor. BCL-XL is the major antiapoptotic survival protein and may be a novel therapeutic target in CML.

Biological activity

In Vitro A-1331852 selectively disrupts BCL-XL–BIM complexes and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells with IC50s in the low nanomolar range but does not affect MEF cells lacking BAK or BAX. In CellTiter-Glo cell viability assay, A-1331852 inhibits NCI-H847, NCI-H1417, SET-2, HEL, OCI-M2 with EC50 values of 3, 7, 80, 120 and 100 nM. In Vivo A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent. Additionally, A-1331852 combines with venetoclax to recapitulate the efficacy of navitoclax in the NCI-H1963.FP5 xenograft model of SCLC. A-1331852 significantly inhibits tumor growth in seven subcutaneous xenograft models of solid tumors, including breast cancer, NSCLC, and ovarian cancer.

Identifiers

SMILES: CC1=C(C=NN1CC12CC3CC(CC(C3)C1)C2)C1=CC=C(N=C1C(O)=O)N1CCC2=C(C1)C(=CC=C2)C(=O)NC1=NC2=CC=CC=C2S1
InChIKey: QCQQONWEDCOTBV-UHFFFAOYSA-N

Specifications

MW (average): 658.8120
Formula: C₃₈H₃₈N₆O₃S
CAS No.: 1430844-80-6
Physical state: Solid
Color: White to light yellow
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℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Leverson JD, et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci Transl Med. 2015 Mar 18;7(279):279ra40.

Same target

Search Bcl-2 Family

Same research area

Search Cancer