2. PROTAC Cell Cycle/DNA Damage
  3. Molecular Glues CDK
  4. CDK2 degrader 3

CDK2 degrader 3 is a selective CDK2 molecular glue-like degrader. CDK2 degrader 3 induces G1 cell cycle arrest in CCNE1-amplified cancer cells. CDK2 degrader 3 is applicable to breast cancer-related research.

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CDK2 degrader 3

CDK2 degrader 3 Chemical Structure

CAS No. : 2862772-71-0

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CDK2 degrader 3 Related Antibodies

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

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Description

CDK2 degrader 3 is a selective CDK2 molecular glue-like degrader. CDK2 degrader 3 induces G1 cell cycle arrest in CCNE1-amplified cancer cells. CDK2 degrader 3 is applicable to breast cancer-related research[1].

IC50 & Target

CDK2

 

In Vitro

CDK2 degrader 3 (compound 1) preferentially forms ternary complexes with CDK2/CCNE1 over CDK1/CCNB1[1].
CDK2 degrader 3 drives preferential ubiquitination of CDK2/cyclin E1 over CDK1/cyclin B1[1].
CDK2 degrader 3 (24 h) potently degrades CDK2 in TOV21G cells with high selectivity over CDK1 and CDK9, with an absDC50 of 8 nM[1].
CDK2 degrader 3 (14 h) potently degrades CDK2 in MKN1 CCNE1amp cells with 95% maximum degradation at an absDC50 of 11 nM[1].
CDK2 degrader 3 (14 h) potently degrades CDK2 in HCC1569 CCNE1amp cells with 94% maximum degradation at an absDC50 of 10 nM[1].
CDK2 degrader 3 (24 h) potently inhibits RB phosphorylation at S807/811 in MKN1 CCNE1amp cells with 96% maximum inhibition at an absIC50 of 27 nM[1].
CDK2 degrader 3 (24 h) inhibits RB phosphorylation at S807/811 in HCC1569 CCNE1amp cells with 87% maximum inhibition at an absIC50 of 34 nM[1].
CDK2 degrader 3 (7 day) potently inhibits proliferation in CCNE1amp cancer cells with significantly lower activity in CCNE1non-amp TOV21G cells, with relIC50 values of 7 nM (MKN1), 16 nM (HCC1569), 28 nM (OVCAR3), and 4000 nM (TOV21G)[1].
CDK2 degrader 3 (500 nM (10x DC90); 24 h) selectively degrades CDK2 in human PBMCs with minimal off-target protein modulation[1].
CDK2 degrader 3 (80 nM; 24 h) suppresses E2F target gene expression in MKN1 cells[1].
CDK2 degrader 3 (1 μM Palbociclib (co-treatment); 24 h) co-degrades CDK2 and cyclin E1 in Palbociclib-adapted MCF7 and Hs578t breast cancer cells[1].

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

CDK2 degrader 3 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Palbociclib-adapted (PA) MCF7 and Hs578t breast cancer cells
Concentration: 1 µM Palbociclib (co-treatment)
Incubation Time: 7 day
Result: Inhibited proliferation in MCF7 PA and Hs578t PA cells, with greater potency compared to activity in CCNE1non-amp cells.

Cell Cycle Analysis[1]

Cell Line: MKN1 CCNE1amp cells
Concentration: 0.0128-5000 nM
Incubation Time: 72 h
Result: Induced G1 cell cycle arrest in a dose-dependent manner.
Achieved a 125x selectivity window between maximum G1 arrest (on-target) and increased G2/M population (off-target).
Molecular Weight

885.47

Formula

C44H53ClN10O6S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1N(C2CCCC2)C3=NC(NC4=C(C=C(C=C4)S(NCCO[C@H]5CC[C@@H](CC5)CN6CCC(C7=CC8=NC=C(N9C(NC(CC9)=O)=O)N8C=C7)CC6)(=O)=O)C)=NC=C3C=C1Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (56.47 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 1.1293 mL 5.6467 mL 11.2934 mL
5 mM 0.2259 mL 1.1293 mL 2.2587 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.91%

SDS (252 KB)

COA (247 KB) HNMR (422 KB) RP-HPLC (252 KB) LCMS (98 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 (protect from light). 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 1.1293 mL 5.6467 mL 11.2934 mL 28.2336 mL
5 mM 0.2259 mL 1.1293 mL 2.2587 mL 5.6467 mL
10 mM 0.1129 mL 0.5647 mL 1.1293 mL 2.8234 mL
15 mM 0.0753 mL 0.3764 mL 0.7529 mL 1.8822 mL
20 mM 0.0565 mL 0.2823 mL 0.5647 mL 1.4117 mL
25 mM 0.0452 mL 0.2259 mL 0.4517 mL 1.1293 mL
30 mM 0.0376 mL 0.1882 mL 0.3764 mL 0.9411 mL
40 mM 0.0282 mL 0.1412 mL 0.2823 mL 0.7058 mL
50 mM 0.0226 mL 0.1129 mL 0.2259 mL 0.5647 mL
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CDK2 degrader 3 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:

CDK2 degrader 32862772-71-0Molecular GluesCDKCyclin dependent kinaseG1 cell cycle arrestCCNE1-amplified cancer cellsCDK2RB-E2F cell cycle pathwayE2F target genePIP4K2CRB phosphorylationcyclin E1Palbociclib-adapted breast cancer cellshuman PBMCsInhibitorinhibitorinhibit

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