BMS-265246
Based on 2 publication(s) in Google Scholar
BMS-265246 is a potent and selective cyclin-dependent kinase CDK1 and CDK2 inhibitor, with IC50 values of 6 and 9 nM, respectively. BMS-265246 inhibits CHI3L1 (chitinase 3-like-1) stimulation of ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases). BMS-265246 can be used for ovarian cancer and COVID-19 research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.59%
- CAS. Nr.: 582315-72-8
- Formel: C18H17F2N3O2
- Molecular Weight:345.34
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) BMS-265246
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Biologische Aktivität
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CDK1/cycB 6 nM (IC50) |
CDK2/Cyc E 9 nM (IC50) |
CDK4/cycD 230 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A2780 | IC50 |
0.76 μM
Compound: 21h
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Cytotoxic effect on ovarian cancer cell line (A2780)
Cytotoxic effect on ovarian cancer cell line (A2780)
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[PMID: 12824044] |
| Sf9 | IC50 |
0.006 μM
Compound: BMS265246
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Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.014 μM
Compound: BMS265246
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Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.222 μM
Compound: BMS265246
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Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.258 μM
Compound: BMS265246
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Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
1.6 μM
Compound: BMS265246
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Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
1.8 μM
Compound: BMS265246
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Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
BMS-265246 binds at the ATP site and shows cytotoxic activity in ovarian cancer cell (A2780), with an IC50 of 0.76 μM[1].
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BMS-265246 (0-10 μM) can dose dependently increase iTreg cell differentiation[2].
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BMS-265246 (9 nM, 24 h) inhibits the ability of CHI3L1 to stimulate epithelial cells ACE2 and SPP[3].
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BMS-265246 (1 μM, 1 h) prevents E2 induction of EGF3, AREG and CXCL12 in MCF7 cells[4].
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BMS-265246 is able to cooperate with Tamoxifen to induce apoptosis in MCF7 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Calu-3 cells
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Concentration:9 nM
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Incubation Time:24 hours
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Result:Abrogated the ability of CHI3L1 (chitinase 3-like-1) to stimulate epithelial cells ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases).
Chemical Information
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CAS. Nr. 582315-72-8
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Appearance Solid
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Molecular Weight 345.34
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Formel C18H17F2N3O2
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Color White to pink
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SMILES
CC1=CC(F)=C(C(C2=CN=C(NN=C3)C3=C2OCCCC)=O)C(F)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Immunity
The transcription factor MEF2C restrains microglial overactivation by inhibiting kinase CDK2. [Abstract]2025 Mar 21:S1074-7613(25)00093-7. PMID: 40139186 -
Lösungsmittel & Löslichkeit
DMSO : 12.5 mg/mL (36.20 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: 2.08 mg/mL (6.02 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Misra RN, Xiao H, Rawlins DB et al. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2405-8. [Content Brief]
[2]. Gu H, et al. Inhibition of CDK2 promotes inducible regulatory T-cell differentiation through TGFβ-Smad3 signaling pathway. Cell Immunol. 2014 Jul;290(1):138-44. [Content Brief]
[3]. Kamle S, et al. Chitinase 3-like-1 is a therapeutic target that mediates the effects of aging in COVID-19. JCI Insight. 2021 Nov 8;6(21):e148749. [Content Brief]
[4]. Scott GK, et al. ERpS294 is a biomarker of ligand or mutational ERα activation and a breast cancer target for CDK2 inhibition. Oncotarget. 2016 Oct 18;8(48):83432-83445. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8957 mL | 14.4785 mL | 28.9570 mL | 72.3924 mL |
| 5 mM | 0.5791 mL | 2.8957 mL | 5.7914 mL | 14.4785 mL | |
| 10 mM | 0.2896 mL | 1.4478 mL | 2.8957 mL | 7.2392 mL | |
| 15 mM | 0.1930 mL | 0.9652 mL | 1.9305 mL | 4.8262 mL | |
| 20 mM | 0.1448 mL | 0.7239 mL | 1.4478 mL | 3.6196 mL | |
| 25 mM | 0.1158 mL | 0.5791 mL | 1.1583 mL | 2.8957 mL | |
| 30 mM | 0.0965 mL | 0.4826 mL | 0.9652 mL | 2.4131 mL |
BMS-265246 Related Classifications
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