2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs CDK
  4. PROTAC CDK2-pRb degrader-1

PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer).

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

PROTAC CDK2-pRb degrader-1

PROTAC CDK2-pRb degrader-1 Chemical Structure

CAS No. : 3030276-48-0

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PROTAC CDK2-pRb degrader-1 Related Antibodies

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Description

PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer)[1].

IC50 & Target

CDK2/cyclinE

 

In Vitro

PROTAC CDK2-pRb degrader-1 (Compound 5) (dose-response concentrations; 24 h) co-degrades CDK2 and cyclin E1 with enhanced activity in CCNE1-amplified human cancer cell lines and restores RB pathway inhibition in albociclib (HY-50767)-adapted breast cancer cells with cyclin E1 overexpression[1].
PROTAC CDK2-pRb degrader-1 (dose-response concentrations; 7 days) exhibits antiproliferative activity in MKN1 and HCC1569 human cancer cell lines that is dependent on CRBN[1].
PROTAC CDK2-pRb degrader-1 (dose-response concentrations; 7 days) exhibits antiproliferative activity in HCC1569 human breast cancer cells that is strictly dependent on functional RB protein[1].

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

PROTAC CDK2-pRb degrader-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MKN1 (CRBNwt, CRBNKO), HCC1569 (CRBNwt, CRBNKO)
Concentration: dose-response concentrations
Incubation Time: 7 days
Result: Lost antiproliferative activity in CRBNKO MKN1 and HCC1569 cells, with proliferation largely restored compared to CRBNwt cells where the degrader potently suppressed growth.

Cell Proliferation Assay[1]

Cell Line: HCC1569 (RBwt, RBKO)
Concentration: dose-response concentrations
Incubation Time: 7 days
Result: Showed >300-fold reduced antiproliferative potency in RBKO HCC1569 cells compared to RBwt cells.
In Vivo

PROTAC CDK2-pRb degrader-1 (50 mg/kg; p.o.; twice daily) achieves nearly 90% pRB inhibition and 85% tumor growth inhibition (near stagnation) in OVCAR3 CCNE1-amplified ovarian cancer xenografts[1].
PROTAC CDK2-pRb degrader-1 (50 mg/kg; p.o.; twice daily) induces tumor stasis or regression; it achieves 90% CDK2 degradation and pRB inhibition in the CCNE1-amplified HCC1569 breast cancer xenograft model[1].
PROTAC CDK2-pRb degrader-1 (50 mg/kg; p.o.; once daily) induces tumor stasis or regression; it achieves 90% CDK2 degradation and pRB inhibition in the CCNE1-amplified MKN1 gastric cancer xenograft model[1].

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

Animal Model: NOD SCID (female)[1]
Dosage: 50 mg/kg
Administration: p.o.; BID
Result: Inhibited nearly 90% of phosphorylated Rb (pRB) in tumor tissue, with decreased rebound of pRB signal at trough compared to PF-07104091 (HY-137894A).
Induced potent tumor growth inhibition (TGI) of 85%.
Animal Model: NOG (female)[1]
Dosage: 15 mg/kg; 30 mg/kg; 50 mg/kg
Administration: p.o.; BID
Result: Achieved sustained 90% CDK2 degradation and 90% pRB inhibition in tumor tissue at 30 and 50 mg/kg BID.
Induced tumor stasis with 95% TGI at 30 mg/kg compared to vehicle.
Induced 5% tumor regression at 50 mg/kg compared to vehicle.
Animal Model: BALB/c Nude (female)[1]
Dosage: 30 mg/kg; 50 mg/kg
Administration: p.o.; QD
Result: Induced 90% CDK2 degradation and 90% pRB inhibition in tumor tissue at 50 mg/kg QD.
Induced tumor stasis (TGI=97%) at 30 mg/kg compared to vehicle.
Induced 47% tumor regression at 50 mg/kg compared to vehicle.
Molecular Weight

830.93

Formula

C40H50F4N8O5S
CAS No.
SMILES

FC(F)(C1=CN=C(NC2=C(C=C(C=C2)S(N[C@H]3CC[C@@H](CC3)CN4CCN(C5=C(C=C(C6C(NC(CC6)=O)=O)C=C5)F)CC4)(=O)=O)C)N=C1N7C[C@@](O)(CCC7)C)F
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Purity & Documentation
References
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PROTAC CDK2-pRb degrader-1 Related Classifications

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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:

PROTAC CDK2-pRb degrader-13030276-48-0PROTACsCDKCyclin dependent kinaseproteasomal degradationCDK2ubiquitinationCCNE1-amplified cancersovarian cancerbreast cancercyclin E1xenograft modelsretinoblastoma protein (Rb)gastric cancerInhibitorinhibitorinhibit

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PROTAC CDK2-pRb degrader-1
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