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A-1331852

Catalog No.GC17513

BCL-XL inhibitor, potent and selective

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A-1331852 Chemical Structure

Cas No.: 1430844-80-6

Size Price Stock Qty
5mg
$90.00
In stock
25mg
$306.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

SCLC and AML cell lines are incubated with increasing concentrations of navitoclax, venetoclax, or A-1155463 for 48 hours before assessing cell viability. Cell killing EC50 values are calculated[1].

Animal experiment:

Mice: The growth inhibition of established tumors in SCID-bg mice is studied. A-1331852 is administered orally daily for 14 days at 25 mg/kg and RP-56976 is administered intravenously at 7.5 mg/kg. The change of tumor volume is monitored daily[1].

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.

Background

Ki: 6 nM for BCL-2 TR-FRET

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

Apoptosis is reported to be regulated by a family of closely related proteins exemplified by B cell lymphoma protein 2 (BCL-2), which is the first discovered family member. BCL-2 family proteins are divided by one to four BCL-2 homology motifs and can be further subdivided into pro- and antiapoptotic subsets.

In vitro: A-1331852 was identified as a potent BCL-XL inhibitor demonstrating cellular activity 10- to 50-fold more potent than its analog A-1155463 and the previouly reported BCL-XL inhibitor, navitoclax, respectively. Moreover, A-1331852 could selectively disrupt BCL-XL–BIM complexes and induce the apoptosis hallmarks in BCL-XL–dependent Molt-4 cells with median IC50 values in the low nanomolar range but did not affect MEF cells without BAK or BAX [1].

In vivo: Previous animal study found that A-1331852 could demonstrate antitumor efficacy in the Molt-4 xenograft model, such as tumor regressions as a single agent. In addition, in the NCI-H1963.FP5 xenograft model of SCLC, it was found that A-1331852 combined with venetoclax was able to recapitulate the efficacy of navitoclax [1].

Clinical trial: Up to now, A-1331852 is still in the preclinical development stage.

Reference:
[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. doi: 10.1126/scitranslmed.aaa4642.

Chemical Properties

Cas No. 1430844-80-6 SDF
Chemical Name 3-(1-(adamantan-1-ylmethyl)-5-methyl-1H-pyrazol-4-yl)-6-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)picolinic acid
Canonical SMILES O=C(C1=NC(N2CC3=C(C=CC=C3C(NC4=NC5=CC=CC=C5S4)=O)CC2)=CC=C1C6=C(C)N(CC78CC9CC(C8)CC(C9)C7)N=C6)O
Formula C38H38N6O3S M.Wt 658.81
Solubility DMF: 5 mg/ml,DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml,DMSO: 2 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.5179 mL 7.5894 mL 15.1789 mL
5 mM 0.3036 mL 1.5179 mL 3.0358 mL
10 mM 0.1518 mL 0.7589 mL 1.5179 mL
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