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> BMS-265246 [582315-72-8]

BMS-265246 [582315-72-8]

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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.

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BMS-265246 Estructura química

BMS-265246 Estructura química

No. CAS : 582315-72-8

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

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Descripciòn

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[1][2][3].

IC50 & Target[1]

CDK1/cycB

6 nM (IC50)

CDK2/Cyc E

9 nM (IC50)

CDK4/cycD

230 nM (IC50)

In Vitro

BMS-265246 binds at the ATP site and shows cytotoxic activity in ovarian cancer cell (A2780), with an IC50 of 0.76 μM[1].
? BMS-265246 (0-10 μM) can dose dependently increase iTreg cell differentiation[2].
? BMS-265246 (9 nM, 24 h) inhibits the ability of CHI3L1 to stimulate epithelial cells ACE2 and SPP[3].
? BMS-265246 (1 μM, 1 h) prevents E2 induction of EGF3, AREG and CXCL12 in MCF7 cells[4].
? 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.

BMS-265246 Related Antibodies

RT-PCR[3]

Cell Line: Calu-3 cells
Concentration: 9 nM
Incubation Time: 24 hours
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).
Peso molecular

345.34

Fòrmula

C18H17F2N3O2
No. CAS

582315-72-8
Appearance

Solid

Color

White to pink

SMILES

CC1=CC(F)=C(C(C2=CN=C(NN=C3)C3=C2OCCCC)=O)C(F)=C1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8957 mL 14.4785 mL 28.9570 mL
5 mM 0.5791 mL 2.8957 mL 5.7914 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, 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.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: 2.08 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.25 mg/mL (3.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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.
Pureza y Documentación

Purity: 98.92%

COA (249 KB) LCMS (94 KB)

Instrucciones de manejo (2659 KB)
Referencias

  • [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]

  • [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.

    [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.

    [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.

    [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.

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
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BMS-265246 Related Classifications

Help & FAQs

Keywords:

BMS-265246582315-72-8BMS265246BMS 265246CDKAngiotensin-converting Enzyme (ACE)Cyclin dependent kinaseiTreg cellA2780MCF7 cellsCalu-3 cellsPyrazolopyridineovarian cancerCOVID-19SARS-CoV-2CHI3L1chitinase 3-like-1Inhibitorinhibitorinhibit

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