product name A-1331852
Description: A-1331852 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases. A-1331852 demonstrated 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
References: Sci Transl Med. 2015 Mar 18;7(279):279ra40; Leukemia. 2016 Jun;30(6):1273-81.
658.81
Formula
C38H38N6O3S
CAS No.
1430844-80-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (151.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: A-1331852 exhibits remarkable potency both as a single agent and in combination with TKIs in killing primary CD34+ CML cell. Also, It has remarkable potency in inducing apoptosis in these cells at low nanomolar concentrations as early as 1 h post-treatment Kinase Assay: Cell Assay: Immunoprecipitation of BCL-XL is carried out in K562 cells, exposed to A-1331852 (100 nM) for 0-2 h, and the eluted complexes are immunoblotted for the indicated proteins. The input cell lysates and the immunodepleted supernatant (labeled as Flow-through) are immunoblotted to check the efficiency of the immunoprecipitation. |
|---|---|
| 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 |
| Animal model | SCID and SCID-bg mice |
| Formulation & Dosage | Formulated in 60% Phosal 50 PG, 27.5 % PEG 400, 10% ethanol, and 2.5% DMSO; 25 mg/kg; Oral gavage |
| References | Sci Transl Med. 2015 Mar 18;7(279):279ra40; Leukemia. 2016 Jun;30(6):1273-81. |
