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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CDK2 degrader 7 Related Antibodies

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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
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.
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
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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CDK2 degrader 7 Related Classifications

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    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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