2. Apoptosis MAPK/ERK Pathway
  3. c-Myc KLF Apoptosis
  4. APTO-253

APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor. APTO-253 has antiarthritic activity.

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

CAS No. : 916151-99-0

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Based on 21 publication(s) in Google Scholar

Other Forms of APTO-253:

APTO-253 Related Antibodies

Top Publications Citing Use of Products

    APTO-253 purchased from MedChemExpress. Usage Cited in: Blood. 2024 Aug 16:blood.2023023644.  [Abstract]

    Cell viability of OCI-AML2 cells expressing either sgLuc or sgPCGF1 was assessed under the treatment of APTO-253 (100 nM; 9 d).

    APTO-253 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 2;14(1):5360.  [Abstract]

    APTO-253 (10 μM) reversed the effects of FAM3A on suppressing the expression of the markers for macrophages (CD68) and osteoblasts (OPN, RUNX2) in VSMCs.

    APTO-253 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 2;14(1):5360.  [Abstract]

    KLF4 inducer APTO-253 (1 μg/g; i.p.; once daily for 4 weeks) significantly abrogated the effects of FAM3A on maintaining the contractile phenotype of VSMCs in aortas from AngII-ApoE−/− murine AAA models.

    APTO-253 purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2021 Apr;80(4):440-450.  [Abstract]

    APTO-253 (1-4 μM) reduced mRNA levels of 8-mix SE-contacted genes (IL-6, CCL5) in stimulated RASFs.

    APTO-253 purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2021 Apr;80(4):440-450.  [Abstract]

    APTO-253 (15 mg/kg; i.v.; twice per day for two consecutive days per week) demonstrated significant therapeutic activity in collagen-induced arthritis (CIA) mice.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor[1][2]. APTO-253 has antiarthritic activity[3].

    IC50 & Target

    c-Myc[1]; KLF4[2]
    In Vitro

    APTO-253 (LOR-253) is an inducer of KLF4. APTO-253 (5 μM) induces KLF4 expression, and enhances apoptosis induced by NSC 119875 in both SKOV3 and OVCAR3 cells. APTO-253 (5 μM) also leads to G1 phase arrest and reduces S and G2/M phase cells in SKOV3 and OVCAR3 cells[1].
    APTO-253 is cytotoxic to Raji and Raji/253R cell lines, with IC50s of 105 ± 2.4 nM and 1387 ± 94 nM, respectively. APTO-253 (0.5 μM) also causes DNA damage in Raji cells. BRCA1/2 deficient cells are hypersensitive to APTO-253. ABCG2 overexpressed HEK-293 cells are resistant to APTO-253 and inhibition of ABCG2 reverses resistance to APTO-253 in Raji/253R[2].
    APTO-253 suppresses the proliferation of acute myeloid leukemia (AML) cell lines and various forms of lymphoma cell lines with IC50s ranging from 57 nM to 1.75 μM. APTO-253 (500 nM) also causes G0/G1 cell cycle arrest, induces apoptosis, and down regulates MYC RNA and protein expression in AML lines. APTO-253 (500 nM) leads to DNA damage response pathways in MV4-11 cells. Futhermore, APTO-253 is a potent stabilizer of Gquadruplex (G4) motifs, and demonstrates the greatest propensity for stabilizing the MYC G4 sequences[3].

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

    APTO-253 Related Antibodies
    In Vivo

    APTO-253 (LOR-253; 15 mg/kg; IV; twice per day for 2 consecutive days per week for 14 days) has antiarthritic activity in a CIA model[3].

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

    Animal Model: DBA/1J male mice (6 weeks) with collagen induced arthritis (CIA)[3]
    Dosage: 15 mg/kg
    Administration: IV; twice per day for 2 consecutive days per week for 14 days
    Result: Demonstrated significant preventive and therapeutic activity on arthritis formation.
    Clinical Trial
    Molecular Weight

    367.38

    Formula

    C22H14FN5
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC(N1)=C(C(N2)=NC3=C2C4=CC=CN=C4C5=NC=CC=C53)C6=C1C=CC(F)=C6
    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 : 25 mg/mL (68.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7220 mL 13.6099 mL 27.2198 mL
    5 mM 0.5444 mL 2.7220 mL 5.4440 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)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.3 mg/mL (6.26 mM); Suspended solution; Need ultrasonic and warming

      This protocol yields a suspended solution of 2.3 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 (23.0 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.
    • Protocol 2

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

      Solubility: 2.08 mg/mL (5.66 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (27.22 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/0.1% Tween-80 in Saline water

      Solubility: 5 mg/mL (13.61 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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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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    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.
    Purity & Documentation

    Purity: 99.74%

    SDS (396 KB)

    COA (258 KB)

    Handling Instructions (2659 KB)
    References

    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
    DMSO 1 mM 2.7220 mL 13.6099 mL 27.2198 mL 68.0494 mL
    5 mM 0.5444 mL 2.7220 mL 5.4440 mL 13.6099 mL
    10 mM 0.2722 mL 1.3610 mL 2.7220 mL 6.8049 mL
    15 mM 0.1815 mL 0.9073 mL 1.8147 mL 4.5366 mL
    20 mM 0.1361 mL 0.6805 mL 1.3610 mL 3.4025 mL
    25 mM 0.1089 mL 0.5444 mL 1.0888 mL 2.7220 mL
    30 mM 0.0907 mL 0.4537 mL 0.9073 mL 2.2683 mL
    40 mM 0.0680 mL 0.3402 mL 0.6805 mL 1.7012 mL
    50 mM 0.0544 mL 0.2722 mL 0.5444 mL 1.3610 mL
    60 mM 0.0454 mL 0.2268 mL 0.4537 mL 1.1342 mL
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    APTO-253 Related Classifications

    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:

    APTO-253916151-99-0LOR-253 LT-253APTO253APTO 253LOR253LOR 253LT253LT 253LT-253c-MycKLFApoptosisMycKrüppel-like factorInhibitorinhibitorinhibit

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