A-1331852

Catalog No.S7801

For research use only.

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.

A-1331852 Chemical Structure

CAS No. 1430844-80-6

Selleck's A-1331852 has been cited by 35 publications

Purity & Quality Control

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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  NGXueZhCeG:ydH;zbZMh[XO|YYm= NITvU|g1QCCq M{\hU4lv\HWlZTDhdI9xfG:|aYOgd5lv\XKpaYP0bYNidGy7IIfpeIghenW6b3zpeIlvcWJiaX6gTGVNKGOnbHzz NViyNYFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5Nlg1QDhpPkK5PVI5PDh6PD;hQi=>
H1299 cells NXTZcZp1SXCxcITvd4l{KGG|c3H5 MmXPNVAxKG6P NVXwWWQ6[SClb33ibY5ifGmxbjDv[kBCNTF{MUC0O|ch[W6mIFGtNVM{OTh3MjDy[ZN2dHSnZDDpckBiKG2jcnvl[EBqdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| MlW2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyN{m4PFcoRjJ6MEe5PFg4RC:jPh?=
CLL MnjMRZBweHSxc3nzJIF{e2G7 M4jGbFQhcA>? Mn7XbY5{\W6|aYTpeoUhfG9iQT2xN|MyQDV{LDDJR|UxRTFwMTFOwG0> NFLa[3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm1OFcyQCd-Mk[5OVQ4OTh:L3G+
MOLT-4 MmfaRZBweHSxc3nzJIF{e2G7 M134PFQhcA>? MYrz[Y5{cXSrdnWgeI8hSS1zM{OxPFUzNCCLQ{WwglYvPyCwTR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl3NEexPEc,OjZ7NUS3NVg9N2F-
H929 MUjBdI9xfG:|aYOgZZN{[Xl? MorLOEBp M{H6SYlve2Wwc3n0bZZmKHSxIFGtNVM{OTh3Mh?= NIC5ZXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm1OFcyQCd-Mk[5OVQ4OTh:L3G+
H1299 MUjBdI9xfG:|aYOgZZN{[Xl? NYrOXVd5PCCq Mni2bY5{\W6|aYTpeoUhfG9iQT2xN|MyQDV{ NYHON|JTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5OVQ4OThpPkK2PVU1PzF6PD;hQi=>
K562 MU\BdI9xfG:|aYOgZZN{[Xl? NEHuUmIzPCCq M13td4V5fHKnbXXsfUBxd3SnboSgbY4hcW6mdXPpcoch[XCxcITvd4l{KGG2IHzve{Bv[W6xbX;sZZIh[2:wY3XueJJifGmxboO= M322UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUi3PVA3Lz5{Nkm4O|kxPjxxYU6=
KCL22 NUTqWXE1SXCxcITvd4l{KGG|c3H5 MYGyOEBp Ml7y[Zh1emWvZXz5JJBwfGWwdDDpckBqdmS3Y3nu[{BieG:ydH;zbZMh[XRibH;3JI5idm:vb3zhdkBkd26lZX70doF1cW:wcx?= NVv2T|N6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5PFc6ODZpPkK2PVg4QTB4PD;hQi=>
MOLT4 MVXDfZRwfG:6aXPpeJkh[XO|YYm= M1rxbmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJkdC2[TDDk[ZBmdmSjboSgUW9NXDRiY3XscJMh[nliY3XscEBj[XOnZDDhd5NigSxiRVO1NEA:KDBwMEC2JO69VS5? M2LFSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUi4N|A3Lz5{Nkm4PFMxPjxxYU6=
Assay
Methods Test Index PMID
Western blot BIM / Bad / Bcl-XL 26987906
Growth inhibition assay Cell viability 28273655
In vivo A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent[1].

Protocol (from reference)

Cell Research:[2]
  • 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.
Animal Research:[1]
  • Animal Models: SCID and SCID-bg mice
  • Dosages: 25 mg/kg
  • Administration: Oral administration

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 658.81
Formula

C38H38N6O3S

CAS No. 1430844-80-6
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Molarity Calculator

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Tech Support

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.

Handling Instructions

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