1. Apoptosis
  2. Bcl-2 Family

A-1331852 

Cat. No.: HY-19741 Purity: 99.21%
Data Sheet SDS 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 $174 In-stock
5 mg $120 In-stock
10 mg $190 In-stock
25 mg $390 In-stock
50 mg $620 In-stock
100 mg $1100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • 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

Ki: less than 10 pM (BCL-XL)[1]

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].

References
Preparing Stock Solutions
Concentration Volume 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.
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]

Mouse: 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

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

Solvent & Solubility

DMSO: ≥ 12 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.21%

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