2. PROTAC Cell Cycle/DNA Damage
  3. Molecular Glues CDK
  4. CDK2 degrader 6

CDK2 degrader 6 is an orally active and potent CDK2 molecular glue degrader with a DC50 of 46.5 nM. CDK2 degrader 6 binds to cereblon and CDK2 to induce ubiquitination and subsequent proteasomal degradation of CDK2. CDK2 degrader 6 modulates cell cycle in breast cancer cells. CDK2 degrader 6 reduces proliferation of breast cancer cells. CDK2 degrader 6 exhibits in vivo antitumor activity in gastric cancer mouse models. CDK2 degrader 6 can be used for the research of breast cancer, gastric cancer.

For research use only. We do not sell to patients.

CDK2 degrader 6

CDK2 degrader 6 Chemical Structure

CAS No. : 3036606-92-2

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CDK2 degrader 6 Related Antibodies

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Description

CDK2 degrader 6 is an orally active and potent CDK2 molecular glue degrader with a DC50 of 46.5 nM. CDK2 degrader 6 binds to cereblon and CDK2 to induce ubiquitination and subsequent proteasomal degradation of CDK2. CDK2 degrader 6 modulates cell cycle in breast cancer cells. CDK2 degrader 6 reduces proliferation of breast cancer cells. CDK2 degrader 6 exhibits in vivo antitumor activity in gastric cancer mouse models. CDK2 degrader 6 can be used for the research of breast cancer, gastric cancer[1].

IC50 & Target[1]

CDK2

46.5 nM (DC50)

In Vitro

CDK2 degrader 6 (compound 6) (24 h) potently induces degradation of CDK2 in CDK2 HiBiT-tagged HEK293 cells, with a 62.0% maximal reduction in CDK2 protein levels and a DC50 of 46.5 nM after 24 hours of treatment[1].
CDK2 degrader 6 (24 h) shows minimal activity in degrading GSPT1 in GSPT1 HiBiT-tagged HEK293 cells, with only a 9.9% maximal reduction in GSPT1 protein levels after 24 hours of treatment[1].
CDK2 degrader 6 (0.316-1000 nM; 7 days) potently inhibits proliferation of MDA-MB-157 breast cancer cells, with a 90% maximal reduction in cell proliferation and an EC50 of 10 nM after 7 days of treatment[1].
CDK2 degrader 6 (152 nM-1000 nM; 24 h) potently induces degradation of CDK2 protein in MDA-MB-157 breast cancer cells, with an 84% maximal reduction in CDK2 levels and a DC50 of 4 nM after 24 hours of treatment[1].
CDK2 degrader 6 (10-1000 nM; 24 h) disrupts the cell cycle of MDA-MB-157 breast cancer cells, causing dose-dependent G1 phase arrest and reduction in S phase cells after 24 hours of treatment at concentrations from 10 nM to 1000 nM[1].

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

CDK2 degrader 6 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-157 breast cancer cells
Concentration: 0.316 nM, 1 nM, 3.16 nM, 10 nM, 31.6 nM, 100 nM, 316 nM, 1000 nM
Incubation Time: 7 days
Result: Reduced cell proliferation by 90% relative to DMSO controls, with an EC50 of 10 nM.

Western Blot Analysis[1]

Cell Line: MDA-MB-157 breast cancer cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 24 h
Result: Induced a maximal 84% reduction in CDK2 protein levels, with a DC50 of 4 nM.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-157 breast cancer cells
Concentration: 10 nM, 100 nM, 1000 nM
Incubation Time: 24 h
Result: Caused a dose-dependent accumulation of cells in the G1 phase (56.3% in DMSO controls vs 65.4% at 1000 nM) and a reduction in cells in the S phase (35.8% in DMSO controls vs 3.1% at 1000 nM).
In Vivo

CDK2 degrader 6 (compound 6) (30-100 mg/kg; p.o.; twice daily; 21 days) produces significant antitumor activity in MKN1 gastric cancer xenografts, with 45% and 47% TGI respectively[1].

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

Animal Model: Mice injected with MKN1[1]
Dosage: 30 mg/kg; 100 mg/kg
Administration: p.o.; twice daily; 21 days
Result: Achieved 45% tumor growth inhibition (TGI) on day 21, with a statistically significant difference compared to vehicle.
Achieved 47% tumor growth inhibition (TGI) on day 21, with a statistically significant difference compared to vehicle.
Molecular Weight

511.44

Formula

C23H22F5N5O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C(CC1)C2=C(F)C=C(N3C[C@H](NC4=NN=C(C56CC(C6)(C(F)(F)F)C5)O4)[C@H]3C)C=C2F)NC1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 15 mg/mL (29.33 mM; Need ultrasonic and warming; 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 1.9553 mL 9.7763 mL 19.5526 mL
5 mM 0.3911 mL 1.9553 mL 3.9105 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 (stored under nitrogen, away from moisture). 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
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 (stored under nitrogen, away from moisture). 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 1.9553 mL 9.7763 mL 19.5526 mL 48.8816 mL
5 mM 0.3911 mL 1.9553 mL 3.9105 mL 9.7763 mL
10 mM 0.1955 mL 0.9776 mL 1.9553 mL 4.8882 mL
15 mM 0.1304 mL 0.6518 mL 1.3035 mL 3.2588 mL
20 mM 0.0978 mL 0.4888 mL 0.9776 mL 2.4441 mL
25 mM 0.0782 mL 0.3911 mL 0.7821 mL 1.9553 mL
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CDK2 degrader 6 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 63036606-92-2Molecular GluesCDKCyclin dependent kinaseMDA-MB-157 breast cancer cellsGSPT1CDK2MKN1 gastric cancer xenograftsHEK293 cellsgastric cancer CDX mouse modelscereblonproteasomal degradationbreast cancer cellscell cycleInhibitorinhibitorinhibit

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