A-1155463 free base · Synonyms: A 1155463 · A1155463

A-1155463, a chemical probe, is a highly potent and selective BCL-XL 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-1155463 structure

CAS No.: 1235034-55-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 490.00	BP-02319-100mg	In stock	Get quote
250 mg	USD 980.00	BP-02319-250mg	In stock	Get quote
500 mg	USD 1,570.00	BP-02319-500mg	In stock	Get quote
1 g	USD 2,500.00	BP-02319-1g	In stock	Get quote
2 g	USD 4,010.00	BP-02319-2g	In stock	Get quote
3 g	USD 4,810.00	BP-02319-3g	In stock	Get quote

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Description

A-1155463, a chemical probe, is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell. A-1155463 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Biological activity

In Vitro A-1155463 shows picomolar binding affinity to BCL-XL (Ki＜0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki= 80 nM) and related proteins BCL-W (Ki= 19 nM) and MCL-1 (Ki> 440 nM) . A-1155463 demonstrates strong growth inhibition of over half of the colorectal cell lines as defined by EC50 values ≤0.5 μM in the presence of 10 % FBS. In Vivo A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses.

Identifiers

SMILES: CN(C)CC#CC1=CC=C(OCCCC2=C(N=C(S2)N2CCC3=C(C2)C(=CC=C3)C(=O)NC2=NC3=CC=CC=C3S2)C(O)=O)C(F)=C1
InChIKey: SOYCFODXNRVBTI-UHFFFAOYSA-N

Specifications

MW (average): 669.7880
Formula: C₃₅H₃₂FN₅O₄S₂
CAS No.: 1235034-55-5
Physical state: Solid
Color: off-white to 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 4℃ 2 years; -20℃ 3 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):279

[2]. Tao ZF, et al. Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity. ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93.

[3]. Zhang H, et al. Genomic analysis and selective small molecule inhibition identifies BCL-X(L) as a critical survival factor in a subset of colorectal cancer. Mol Cancer. 2015 Jul 2;14:126.

Same target

Search Bcl-2 Family

Same research area

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