2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK2 degrader 7

CDK2 degrader 7 is an orally active CDK2 degrader, with DC50 values of 13 nM (MKN1cells) and 17 nM (TOV21G cells). CDK2 degrader 7 induces G1 phase arrest in MKN1 cells. CDK2 degrader 7 achieves tumor stasis in HCC1569 (CCNE1-amplified) xenograft models. CDK2 degrader 7 can be used for the study of CCNE1-amplified cancers.

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CDK2 degrader 7

CDK2 degrader 7 Chemical Structure

CAS No. : 3030279-55-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

CDK2 degrader 7 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 7 is an orally active CDK2 degrader, with DC50 values of 13 nM (MKN1cells) and 17 nM (TOV21G cells). CDK2 degrader 7 induces G1 phase arrest in MKN1 cells. CDK2 degrader 7 achieves tumor stasis in HCC1569 (CCNE1-amplified) xenograft models. CDK2 degrader 7 can be used for the study of CCNE1-amplified cancers[1].

IC50 & Target[1]

CDK2

13 nM (DC50, MKN1cells)

CDK2

17 nM (DC50, TOV21G cells)

CDK1

2130 nM (DC50)

In Vitro

CDK2 degrader 7 (Compound 37) exhibits potent CDK2 degradation activity in MKN1 (CCNE1-amplified) and TOV21G (CCNE1-nonamplified) cells, with DC50 values of 13 nM and 17 nM[1].
CDK2 degrader 7 displays potent antiproliferative activity against MKN1 (CCNE1-amplified) cells with an IC50 of 9 nM, while showing weak activity against TOV21G (CCNE1-nonamplified) cells with an IC50 of 5760 nM[1].
CDK2 degrader 7 (4.88-5000 nM , 72 h) induces maximum G1 phase arrest (on-target effect) at 78 nM and shows off-target G2/M accumulation at 2500 nM in MKN1 cells[1].

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

CDK2 degrader 7 Related Antibodies
Parmacokinetics
Species Dose Route CL Vss T1/2 Tmax Cmax AUClast F
Dog[1] 0.1 mg/kg i.v. 0.1 mL/min/kg 3.9 L/kg 14.4 h / / / /
Dog[1] 1 mg/kg p.o. / / / 4.0 h 0.025 μM 0.557 μM·h 12 %
Monkey[1] 0.07 mg/kg i.v. 9.1 mL/min/kg 5.7 L/kg 6.7 h / / / /
Monkey[1] 1 mg/kg p.o. / / / 4.0 h 0.014 μM 3.63 μM·h 21 %
Rat[1] 10 mg/kg p.o. / / / 2.0 h 0.261 μM 3.63 μM·h 21 %
Rat[1] 2 mg/kg i.v. 10 mL/min/kg 5 L/kg 6.7 h / / / /
In Vivo

CDK2 degrader 7 (Compound 37) (10-50 mg/kg, p.o., once or twice daily, 28 days) demonstrates robust antitumor activity in HCC1569 (CCNE1-amplified) xenograft mode [1].

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

Animal Model: HCC1569 human breast carcinoma cells (6 × 106 cells + Matrigel in 0.2 mL RPMI 1640 medium) were subcutaneously implanted into the central right flank of 7-day acclimated female NOG mice[1]
Dosage: 10 mg/kg, 25 mg/kg, 50 mg/kg
Administration: p.o., once or twice daily, 28 days
Result: Achieved tumor stasis in HCC1569 (CCNE1-amplified) xenograft model.
Molecular Weight

852.89

Formula

C39H46F6N8O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(NC2=NC=C(C(F)(F)F)C(N3C[C@@](C)(O)CCC3)=N2)C(F)=C1)(N[C@H]4[C@@H](F)CN(CC5CCN(C6=CC=C(C(CC7)C(NC7=O)=O)C=C6F)CC5)CC4)=O
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 (117.25 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 1.1725 mL 5.8624 mL 11.7248 mL
5 mM 0.2345 mL 1.1725 mL 2.3450 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.

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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 (2.93 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.93 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:

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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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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.
Purity & Documentation
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 1.1725 mL 5.8624 mL 11.7248 mL 29.3121 mL
5 mM 0.2345 mL 1.1725 mL 2.3450 mL 5.8624 mL
10 mM 0.1172 mL 0.5862 mL 1.1725 mL 2.9312 mL
15 mM 0.0782 mL 0.3908 mL 0.7817 mL 1.9541 mL
20 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4656 mL
25 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1725 mL
30 mM 0.0391 mL 0.1954 mL 0.3908 mL 0.9771 mL
40 mM 0.0293 mL 0.1466 mL 0.2931 mL 0.7328 mL
50 mM 0.0234 mL 0.1172 mL 0.2345 mL 0.5862 mL
60 mM 0.0195 mL 0.0977 mL 0.1954 mL 0.4885 mL
80 mM 0.0147 mL 0.0733 mL 0.1466 mL 0.3664 mL
100 mM 0.0117 mL 0.0586 mL 0.1172 mL 0.2931 mL
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CDK2 degrader 7 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 73030279-55-8CDKCyclin dependent kinaseMKN1 cellsTOV21G cellscancerHCC1569Inhibitorinhibitorinhibit

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