2. Cell Cycle/DNA Damage
  3. CDK
  4. INX-315

INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research.

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

CAS No. : 2745060-92-6

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Customer Review

Based on 6 publication(s) in Google Scholar

INX-315 Related Antibodies

Top Publications Citing Use of Products

    INX-315 purchased from MedChemExpress. Usage Cited in: EMBO J. 2025 Aug;44(15):4378-4405.  [Abstract]

    Wild-type hTERT-RPE1 FUCCI cells were synchronized in G2 with a CDK1 inhibitor for 18 h, treated for 8 h with 100 nM of the CDK2 inhibitor PF-06873600 (CDK2i), 500 nM, 1 µM, or 2 µM of the alternative CDK2 inhibitor INX-315 (CDK2i-2), or 5 µM of the pan-CDK inhibitor flavopiridol (panCDKi), or DMSO (–), and then analyzed by Western blotting for cell cycle markers.

    INX-315 purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Jul 7;9(1):223.  [Abstract]

    INX-315 (72 h) inhibited the cell growth of CDK2-knockdown PC3, ResA, and 22RV1 cells.

    INX-315 purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Jul 7;9(1):223.  [Abstract]

    INX-315 (2 μM, 6 h) inhibited the mRNA expression of ASPM, CDC20, DLGAP5, and KIF18A in CDK2-knockdown PC3, ResA, and 22RV1 cells.

    INX-315 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Nov 15:2024.11.11.623139.  [Abstract]

    Continuous Palbociclib (1 μM) and fulvestrant (500 nM) treatment for 20 days significantly reduced resistant-cell growth compared to palbociclib discontinuation, fulvestrant alone, or fulvestrant plus INX-315 (100 nM).

    INX-315 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Nov 15:2024.11.11.623139.  [Abstract]

    Treatment with INX-315 (0.1 μM, 24 h) initially inhibited CDK2 or CDK4/6 activity within 1–2 h after drug treatment, but reactivation occurred regardless of cyclin E1 or A2 overexpression in MCF7 cells.

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

    • Biological Activity

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    Description

    INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research[1].

    IC50 & Target

    CDK2[1].
    In Vitro

    INX-315 (30-300 nM, 24 hours) inhibits cell cycle progression in OVCAR3 and MKN1 cells by reducing retinoblastoma protein (Rb) phosphorylation[1].
    INX-315 (0.3 nM to 10 μM, 6 days) inhibits cell proliferation in CCNE1-amplified ovarian carcinoma cell line[1].

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

    INX-315 Related Antibodies

    Western Blot Analysis[1]

    Cell Line: OVCAR3 (CCNE1-amplified ovarian carcinoma cells) and MKN1 (gastric cancer cells)
    Concentration: 30, 100, 300 nM
    Incubation Time: 24 h
    Result: Reduced the phosphorylation level of Rb and the expression level of Cyclin A2.

    Cell Viability Assay[1]

    Cell Line: OVCAR-3 (CCNE1-amplified ovarian carcinoma cells)
    Concentration: 0.3 nM to 10 μM
    Incubation Time: 6 days
    Result: Decreased cell viability in a dose-dependent manner.
    In Vivo

    INX-315 (100 mg/kg, p.o., twice daily for 56 days) effectively inhibits tumor growth in a gastric adenocarcinoma BALB/c nude mouse model[1].
    INX-315 (100 mg/kg twice daily or 200 mg/kg once daily, i.p.) demonstrates significant tumor inhibition in the OVCAR3 ovarian cancer CDX model with good tolerance[2].
    INX-315 (100 mg/kg twice daily, i.p.) demonstrates significant antitumor activity in the GA0103 gastric cancer PDX model with good tolerance[2].

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

    Animal Model: OVCAR3 ovarian cancer CDX model constructed by injecting OVCAR3 ovarian cancer cell line into immunodeficient mice[2]
    Dosage: 100 or 200 mg/kg
    Administration: Intraperitoneal injection (i.p.), 100 mg/kg twice daily or 200 mg/kg once daily for up to 42 days
    Result: Resulted in tumor stasis (100 mg/kg twice daily), achieved 89% tumor growth inhibition (TGI), and did not cause significant weight loss (200 mg/kg once daily).
    Animal Model: GA0103 gastric cancer PDX model constructed by injecting patient-derived GA0103 gastric cancer tumor into immunodeficient mice[2]
    Dosage: 100 mg/kg
    Administration: Intraperitoneal injection (i.p.), twice daily for 56 days
    Result: Resulted in tumor stasis and did not cause significant weight loss.
    Animal Model: CCNE1-amplified gastric adenocarcinoma PDX (GA0103) in BALB/c nude mice model[1]
    Dosage: 25, 50, 100 mg/kg
    Administration: Oral gavage (p.o.), twice daily, for 56 days
    Result: inhibited the growth of tumor in a dose-dependent manner, with 100 mg/kg group showing tumor regression.
    Clinical Trial
    Molecular Weight

    427.48

    Formula

    C19H21N7O3S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NN1)C2(CCCCC2)N(C1=C3)C4=C3C=NC(NC5=CC=C(S(=O)(N)=O)C=C5)=N4
    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 : 100 mg/mL (233.93 mM; Need ultrasonic; 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 2.3393 mL 11.6965 mL 23.3929 mL
    5 mM 0.4679 mL 2.3393 mL 4.6786 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: ≥ 2.5 mg/mL (5.85 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.85 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Number of animals

    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.
    Purity & Documentation

    Purity: 99.75%

    SDS (251 KB)

    COA (262 KB) HNMR (262 KB) RP-HPLC (245 KB) LCMS (94 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 2.3393 mL 11.6965 mL 23.3929 mL 58.4823 mL
    5 mM 0.4679 mL 2.3393 mL 4.6786 mL 11.6965 mL
    10 mM 0.2339 mL 1.1696 mL 2.3393 mL 5.8482 mL
    15 mM 0.1560 mL 0.7798 mL 1.5595 mL 3.8988 mL
    20 mM 0.1170 mL 0.5848 mL 1.1696 mL 2.9241 mL
    25 mM 0.0936 mL 0.4679 mL 0.9357 mL 2.3393 mL
    30 mM 0.0780 mL 0.3899 mL 0.7798 mL 1.9494 mL
    40 mM 0.0585 mL 0.2924 mL 0.5848 mL 1.4621 mL
    50 mM 0.0468 mL 0.2339 mL 0.4679 mL 1.1696 mL
    60 mM 0.0390 mL 0.1949 mL 0.3899 mL 0.9747 mL
    80 mM 0.0292 mL 0.1462 mL 0.2924 mL 0.7310 mL
    100 mM 0.0234 mL 0.1170 mL 0.2339 mL 0.5848 mL
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    INX-315 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:

    INX-3152745060-92-6INX315INX 315CDKCyclin dependent kinaseOVCAR3cancertumorMKN1Inhibitorinhibitorinhibit

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