1. Apoptosis
  2. Bcl-2 Family

A-1331852 

Cat. No.: HY-19741 Purity: 99.21%
Handling Instructions

A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM.

For research use only. We do not sell to patients.

A-1331852 Chemical Structure

A-1331852 Chemical Structure

CAS No. : 1430844-80-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 209 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
25 mg USD 468 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 744 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 1320 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM.

IC50 & Target[1]

Bcl-xL

0.01 nM (Ki)

Bcl-W

4 nM (Ki)

Bcl-2

6 nM (Ki)

Mcl-1

142 nM (Ki)

In Vitro

A-1331852 selectively disrupts BCL-XL–BIM complexes and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells with IC50s in the low nanomolar range but does not affect MEF cells lacking BAK or BAX. In CellTiter-Glo cell viability assay, A-1331852 inhibits NCI-H847, NCI-H1417, SET-2, HEL, OCI-M2 with EC50 values of 3, 7, 80, 120 and 100 nM[1].

In Vivo

A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent. Additionally, A-1331852 combines with venetoclax to recapitulate the efficacy of navitoclax in the NCI-H1963.FP5 xenograft model of SCLC. A-1331852 significantly inhibits tumor growth in seven subcutaneous xenograft models of solid tumors, including breast cancer, NSCLC, and ovarian cancer[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 12 mg/mL (18.21 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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 docetaxel is administered intravenously at 7.5 mg/kg. The change of tumor volume is monitored daily[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

658.81

Formula

C₃₈H₃₈N₆O₃S

CAS No.

1430844-80-6

SMILES

O=C(C1=NC(N2CC3=C(C=CC=C3C(NC4=NC5=CC=CC=C5S4)=O)CC2)=CC=C1C6=C(C)N(CC7(C8)CC9CC8CC(C9)C7)N=C6)O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
A-1331852
Cat. No.:
HY-19741
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A-1331852

Cat. No.: HY-19741