INX-315
Based on 6 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.75%
- No. CAS: 2745060-92-6
- Fòrmula: C19H21N7O3S
- Peso molecular:427.48
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) INX-315
More- NPJ Precis Oncol. 2025 Jul 7;9(1):223. [Abstract]
- NPJ Breast Cancer. 2025 Dec 3;11(1):135. [Abstract]
- EMBO J. 2025 Aug;44(15):4378-4405. [Abstract]
- Sci Signal. 2025 Nov 25;18(914):eadv0415. [Abstract]
- bioRxiv. 2025 Nov 3:2025.11.02.685764. [Abstract]
- bioRxiv. 2024 Nov 15:2024.11.11.623139. [Abstract]
-
Cell Proliferation/Viability Assay
-
RT-PCR
-
WB
-
Cell Proliferation/Viability Assay
-
Bio/Physico-chemical Assay
Actividad biológica
CDK2[1].
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.
-
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 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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 2745060-92-6
-
Appearance Solid
-
Peso molecular 427.48
-
Fòrmula C19H21N7O3S
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
-
Journal Impact Factor
-
Most Recent
-
NPJ Precis Oncol
Transcriptional profiling clarifies a program of enzalutamide extreme non-response in lethal prostate cancer. [Abstract]2025 Jul 7;9(1):223. PMID: 40624104
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.
-
NPJ Breast Cancer
CDK2 inhibition enhances CDK4/6 inhibitor antitumor activity in comprehensive breast cancer PDX model screen. [Abstract]2025 Dec 3;11(1):135. PMID: 41339342 -
EMBO J
2025 Aug;44(15):4378-4405. PMID: 40551011
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.
-
Sci Signal
p16 expression confers sensitivity to CDK2 inhibitors in cyclin E1-driven ovarian cancers. [Abstract]2025 Nov 25;18(914):eadv0415. PMID: 41289358 -
bioRxiv
2025 Nov 3:2025.11.02.685764. PMID: 41279360 -
bioRxiv
Therapeutic benefits of maintaining CDK4/6 inhibitors and incorporating CDK2 inhibitors beyond progression in breast cancer. [Abstract]2024 Nov 15:2024.11.11.623139. PMID: 39605351
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.
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
-
Ficha de datos (287 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
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 |