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

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

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CAS 番号 : 1430844-80-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 209 在庫あり
Solution
10 mM * 1 mL in DMSO USD 209 在庫あり
Solid
1 mg $70 在庫あり
5 mg $144 在庫あり
10 mg $228 在庫あり
25 mg $468 在庫あり
50 mg $700 在庫あり
100 mg $995 在庫あり
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カスタマーレビュー

Based on 52 publication(s) in Google Scholar

A-1331852 関連抗体

Top Publications Citing Use of Products

顧客検証

IHC
In Vivo Imaging
Cell Proliferation/Viability Assay
WB
Bio/Physico-chemical Assay
Flow Cytometry

    A-1331852 purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2024 Jul;5(7):1082-1101.  [Abstract]

    Growth inhibition curves (left panel), IC50 values, and AUCs (right panel) of OCI-AML2 cells treated with DMSO or 500nM ARM165 in combination with increasing doses (10-10000 nM）of either venetoclax, S63845, WEHI-539 and A-1331852. Error bars represent mean ± SD of three biological replicates composed of seven technical repeats after three days of seeding.

    A-1331852 purchased from MedChemExpress. Usage Cited in: Cell. 2022 Apr 28;185(9):1521-1538.e18.  [Abstract]

    Sensitivity of resting and pre-activated NK cells to BCL-XL inhibitor (A-1331852; 0-4096 nM; 24 h), as measured by annexin V staining.

    A-1331852 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2023 Feb 1:554:216028.  [Abstract]

    Xenotransplanted zebrafish larvae were treated with A-1331852 (10 μM; 48 h) (1 dpi - 3 dpi). Dot plots show relative changes of tumor area (3 dpi/1 dpi).

    A-1331852 purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2021 Jan;2(1):34-48.  [Abstract]

    Representative cleaved caspase-3 staining and quantification of cleaved caspase-3-positive area in PDX 14–07 tumors treated with vehicle (n=21), abemaciclib (n=18), A-1331852 (25 mg/kg, p.o., every 12 hours, 3 doses in total) (n=15), or the combination (n=18). Mean ± s.d. of positively stained area are shown. P values were determined by Kruskal-Wallis, Dunn’s multiple comparisons test. Scale bars represent 100 μm.

    A-1331852 purchased from MedChemExpress. 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.

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

    Immunoblot with cell lysates collected after 48 h treatment with DMSO, single drugs: S63845 (156 nM) and A-1331852 (156 nM), or combinations, and probed for PARP. Both combinations increased the cleaved product of PARP. Molecular weight markers are in kDa.

    Bcl-2 Family アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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)

    Cellular Effect
    Cell Line Type Value Description References
    MOLT-4 EC50
    6 nM
    Compound: 33; A-1331852
    Cytotoxicity against human Bcl-XL dependant MOLT4 cells by cell based assay
    Cytotoxicity against human Bcl-XL dependant MOLT4 cells by cell based assay
    		[PMID: 26988306]
    MOLT-4 EC50
    6 nM
    Compound: A-1331852
    Antiproliferative activity against Bcl-xl dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay
    Antiproliferative activity against Bcl-xl dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay
    		[PMID: 25787766]
    MOLT-4 EC50
    6.3 nM
    Compound: 13, A-1331852
    Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay
    Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay
    		[PMID: 33062160]
    MOLT-4 EC50
    > 5000 nM
    Compound: A-1331852
    Antiproliferative activity against Bcl-2 dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay
    Antiproliferative activity against Bcl-2 dependent human MOLT-4 cells assessed as reduction in cell viability by measuring effect concentration by CellTiter-Glo reagent based assay
    		[PMID: 25787766]
    RS4-11 EC50
    > 5 μM
    Compound: 33; A-1331852
    Cytotoxicity against human Bcl-2 dependant RS4:11 cells by cell based assay
    Cytotoxicity against human Bcl-2 dependant RS4:11 cells by cell based assay
    		[PMID: 26988306]
    RS4-11 EC50
    > 5000 nM
    Compound: 13, A-1331852
    Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay
    Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay
    		[PMID: 33062160]
    体外実験

    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].

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

    A-1331852 関連抗体
    体内実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    658.81

    分子式

    C38H38N6O3S
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 50 mg/mL (75.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

    H2O : < 0.1 mg/mL (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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

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    体積 （開始）

    V1

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    濃度 （終了）

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    体積 （終了）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  2.5% DMSO    10% Ethanol    27.5% PEG300    60% Phosal 50 PG

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

    • Protocol 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

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.93%

    COA (262 KB) LCMS (105 KB) Elemental Analysis Report (119 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 1.5179 mL 7.5894 mL 15.1789 mL 37.9472 mL
    5 mM 0.3036 mL 1.5179 mL 3.0358 mL 7.5894 mL
    DMSO 10 mM 0.1518 mL 0.7589 mL 1.5179 mL 3.7947 mL
    15 mM 0.1012 mL 0.5060 mL 1.0119 mL 2.5298 mL
    20 mM 0.0759 mL 0.3795 mL 0.7589 mL 1.8974 mL
    25 mM 0.0607 mL 0.3036 mL 0.6072 mL 1.5179 mL
    30 mM 0.0506 mL 0.2530 mL 0.5060 mL 1.2649 mL
    40 mM 0.0379 mL 0.1897 mL 0.3795 mL 0.9487 mL
    50 mM 0.0304 mL 0.1518 mL 0.3036 mL 0.7589 mL
    60 mM 0.0253 mL 0.1265 mL 0.2530 mL 0.6325 mL
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    A-1331852 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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.

    Keywords:

    A-13318521430844-80-6A1331852A 1331852Bcl-2 FamilyInhibitorinhibitorinhibit

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    製品名:
    A-1331852
    製品番号:
    HY-19741
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