A-1331852

For research use only.

Catalog No.S7801

28 publications

A-1331852 Chemical Structure

CAS No. 1430844-80-6

A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 419 In stock
USD 197 In stock
USD 989 In stock
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Selleck's A-1331852 has been cited by 28 publications

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Choose Selective Bcl-2 Inhibitors

Biological Activity

Description A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases.
Targets
Bcl-xL [1]
(Cell-free assay)
<0.01 nM(Ki)
In vitro

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[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEL cells  MYHBdI9xfG:|aYOgZZN{[Xl? MV[0PEBp MmTWbY5lfWOnIHHwc5B1d3OrczDzfY5memerc4TpZ4FtdHlid3n0bEBzfXixbHn0bY5q[iCrbjDISWwh[2WubIO= NUXJWVUxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5Nlg1QDhpPkK5PVI5PDh6PD;hQi=>
H1299 cells NHnlSGZCeG:ydH;zbZMh[XO|YYm= MmjQNVAxKG6P MonYZUBkd22kaX7heIlwdiCxZjDBMVEzOTB2N{egZY5lKEFvMUOzNVg2OiC{ZYP1cJRm\CCrbjDhJI1iemunZDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ M2T6VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEe5PFg4Lz5{OEC3PVg5PzxxYU6=
CLL M3vZdmFxd3C2b4Ppd{Bie3OjeR?= M1joRlQhcA>? MUHpcpNmdnOrdHn2[UB1dyCDLUGzN|E5PTJuIFnDOVA:OS5zIN88US=> M1Tqd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUW0O|E5Lz5{Nkm1OFcyQDxxYU6=
MOLT-4 MXTBdI9xfG:|aYOgZZN{[Xl? M2n0[|QhcA>? MVnz[Y5{cXSrdnWgeI8hSS1zM{OxPFUzNCCLQ{WwglYvPyCwTR?= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl3NEexPEc,OjZ7NUS3NVg9N2F-
H929 MVjBdI9xfG:|aYOgZZN{[Xl? NVnCdHFTPCCq M4LldIlve2Wwc3n0bZZmKHSxIFGtNVM{OTh3Mh?= NHHyNXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm1OFcyQCd-Mk[5OVQ4OTh:L3G+
H1299 NGTJXVZCeG:ydH;zbZMh[XO|YYm= M1vGNVQhcA>? NHXDPGZqdnOnboPpeIl3\SC2bzDBMVE{OzF6NUK= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl3NEexPEc,OjZ7NUS3NVg9N2F-
K562 Mo\MRZBweHSxc3nzJIF{e2G7 NV3pPIZyOjRiaB?= NXu1cnhl\Xi2cnXt[Yx6KHCxdHXueEBqdiCrbnT1Z4lv\yCjcH;weI9{cXNiYYSgcI94KG6jbn;tc4xieiClb37j[Y51emG2aX;udy=> NH:0OVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm4O|kxPid-Mk[5PFc6ODZ:L3G+
KCL22 NEjVXm1CeG:ydH;zbZMh[XO|YYm= MV6yOEBp NW\FT2w1\Xi2cnXt[Yx6KHCxdHXueEBqdiCrbnT1Z4lv\yCjcH;weI9{cXNiYYSgcI94KG6jbn;tc4xieiClb37j[Y51emG2aX;udy=> M3HheVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUi3PVA3Lz5{Nkm4O|kxPjxxYU6=
MOLT4 MV3DfZRwfG:6aXPpeJkh[XO|YYm= M4X0OWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJkdC2[TDDk[ZBmdmSjboSgUW9NXDRiY3XscJMh[nliY3XscEBj[XOnZDDhd5NigSxiRVO1NEA:KDBwMEC2JO69VS5? NIPhVo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm4PFMxPid-Mk[5PFg{ODZ:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
BIM / Bad / Bcl-XL; 

PubMed: 26987906     


Immunoprecipitation of BCL-XL was carried out in K562 cells, exposed to A-1331852 (100 nm) for 0–2 h, and the eluted complexes were immunoblotted for the indicated proteins. The input cell lysates and the immunodepleted supernatant (labeled as Flow-through) were immunoblotted to check the efficiency of the immunoprecipitation. BC represents beads control. 

26987906
Growth inhibition assay
Cell viability; 

PubMed: 28273655     


A1331852 selectively reduces senescent but not proliferating HUVECs and IMR90 cell numbers (crystal violet). The red lines denote cell numbers at plating on day 0 of senescent and non-senescent cells, both set to 100%. HUVEC and IMR90 data are means±SEM of 5 replicates at each drug concentration. Preadipocyte data are means±SEM of 5 replicates from each of 4 different subjects at each concentration.

28273655
In vivo A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent[1].

Protocol

Cell Research:[2]
- Collapse
  • Cell lines: K562 cells
  • Concentrations: 100 nM
  • Incubation Time: 0-2 h
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: SCID and SCID-bg mice
  • Dosages: 25 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (151.78 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 658.81
Formula

C38H38N6O3S

CAS No. 1430844-80-6
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C=NN1CC23CC4CC(C2)CC(C4)C3)C5=C(N=C(C=C5)N6CCC7=C(C6)C(=CC=C7)C(=O)NC8=NC9=CC=CC=C9S8)C(=O)O

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID