1. Apoptosis
  2. Bcl-2 Family
  3. S63845

S63845 

Cat. No.: HY-100741 Purity: 99.13%
COA Handling Instructions

S63845 est un inhibiteur puissant et sélectif de la leucémie myéloïde 1 (MCL1) avec un Kd de 0,19 nM pour MCL1 humain.

S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1.

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

S63845 Chemical Structure

S63845 Chemical Structure

CAS No. : 1799633-27-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 274 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 274 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
25 mg USD 540 In-stock
Estimated Time of Arrival: December 31
50 mg USD 780 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 48 publication(s) in Google Scholar

Top Publications Citing Use of Products

45 Publications Citing Use of MCE S63845

WB
Cell Viability Assay

    S63845 purchased from MCE. Usage Cited in: Clin Cancer Res. 2018 Nov 1;24(21):5458-5470.  [Abstract]

    Primary LuCaP35CR and LuCaP70CR cultures are treated with ABT-263 alone, S63845 alone, or combination for 4 hours in 2D culture. The cell lysates then are immunoblotted for indicated proteins.

    S63845 purchased from MCE. Usage Cited in: Clin Res Hepatol Gas. 2019 Jun;43(3):292-300.  [Abstract]

    S63845 and A-1210477 trigger apoptosis signaling and reduce the levels of putative stem biomarkers in HCC cell lines.

    S63845 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. shBCLXL (in presence of S63845) shows significant reduction in cell viability during 48 h drug treatment.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1[1].

    IC50 & Target[1]

    MCL1

    0.19 nM (Kd)

    In Vitro

    The pro-survival protein myeloid cell leukemia 1 (MCL1) is over expressed in many cancers. S63845 is a small molecule that specifically binds with high affinity to the BH3-binding groove of MCL1. S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. The activity of S63845 is next evaluated in a panel of eight AML cell lines: all lines are sensitive to S63845 (IC50=4-233 nM)[1].

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

    In Vivo

    S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Intravenously injected (i.v.) S63845 exerts dose-dependent anti-tumour activity in human multiple myeloma (H929 and AMO1) xenografts in immunocompromised mice, with maximal tumour growth inhibition of 114% in the AMO1 model and 103% in the H929 model. At 25 mg/kg, S63845 induces complete regression in 7 out of 8 of the mice at 100 days after treatment in the AMO1 model[1].

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

    Molecular Weight

    829.26

    Formula

    C39H37ClF4N6O6S

    CAS No.
    SMILES

    CC(C(Cl)=C(OCCN1CCN(C)CC1)C=C2)=[[email protected]@]2[[email protected]]3=C(C4=CC=C(F)O4)SC5=NC=NC(O[[email protected]](CC6=C(OCC7=CC=NN7CC(F)(F)F)C=CC=C6)C(O)=O)=C53

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (40.19 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2059 mL 6.0295 mL 12.0589 mL
    5 mM 0.2412 mL 1.2059 mL 2.4118 mL
    10 mM 0.1206 mL 0.6029 mL 1.2059 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  50% PEG300    50% saline

      Solubility: 5 mg/mL (6.03 mM); Clear solution; Need ultrasonic

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (2.51 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (2.51 mM); Clear solution

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

    Purity: 99.94%

    References
    Kinase Assay
    [1]

    10 mM HEPES pH 7.4, 175 mM NaCl, 25 μM EDTA, 1 mM TCEP, 0.01% P20 and 1% DMSO is used as a running buffer. The ligand surface is generated using double His-tagged proteins. Serial dilutions of the compound in buffer are injected over the protein surface. All sample measurements are performed at a flow rate of 30 μL per min (injection time 120 s, dissociation time 360 s). The sensor surface is regenerated by consecutive injections of 0.35 M EDTA pH 8.0 with 0.1 mg/mL trypsin, 0.5 M imidazole and 45% DMSO (60 s, 15 μL per min)[1].

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

    Cell Assay
    [1]

    Cells are treated with increasing doses of S63845 (typically 0.008, 0.025, 0.04, 0.2, 1, 5 μM) for 24 h. Cells are stained with Annexin V-FITC and propidium iodide, analysed on a FACS Calibur and live cells are recorded. Data are presented as per cent cell death induction relative to cells cultured in medium alone[1].

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

    Animal Administration
    [1]

    Mice: S63845 is formulated extemporaneously in 25 mM HCl, 20% 2-hydroxy propyl β -cyclo dextrin 20% and administrated at the 6.25, 12.5, 25 mg/kg for 0, 20, 40, 60, 80 days. Tumour growth inhibition (TGImax) is calculated[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:
    S63845
    Cat. No.:
    HY-100741
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