1. Apoptosis
  2. Bcl-2 Family
  3. A-1331852

A-1331852 

Cat. No.: HY-19741 Purity: 99.65%
COA 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  
Solution
10 mM * 1 mL in DMSO USD 209 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 209 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
25 mg USD 468 In-stock
Estimated Time of Arrival: December 31
50 mg USD 744 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 19 publication(s) in Google Scholar

Top Publications Citing Use of Products

    A-1331852 purchased from MCE. Usage Cited in: Cell Death Dis. 2020 Jun 8;11(6):443.  [Abstract]

    In A375 cells, knockdown (KD) of MCL1 (shMCL1), BCL2 (shBCL2), BCLW (shBCLW), and BCLXL (shBCLXL) lines are created by shRNA technology. shMCL1 (in presence of ABT-263 or A-1331852) shows significant reduction in cell viability during 48 h drug treatment.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    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].

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

    Molecular Weight

    658.81

    Formula

    C38H38N6O3S

    CAS No.
    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (75.89 mM)

    Ethanol : 4 mg/mL (6.07 mM; ultrasonic and warming and heat to 60°C)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble)

    *"≥" 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.
    In Vivo:
    • 1.

      Add each solvent one by one:  2.5% DMSO    10% ethanol    27.5% PEG 300    60% Phosal 50 PG

      Solubility: ≥ 2.5 mg/mL (3.79 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.08 mg/mL (3.16 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.08 mg/mL (3.16 mM); Suspended solution; Need ultrasonic

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (3.16 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.65%

    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 RP-56976 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
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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