CCNE1 degrader-2
CCNE1 degrader-2 is an orally active CCNE1 degrader with a paDC50 of 7.7 nM. CCNE1 degrader-2 promotes the targeted degradation of Cyclin E1 protein. CCNE1 degrader-2 inhibits tumor cell proliferation and exerts antitumor activity in CDX in vivo models. CCNE1 degrader-2 is used in research on cancers such as ovarian cancer and breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3133169-21-5
- Formula: C30H27FN4O5
- Molecular Weight:542.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CCNE1 |
In Vitro
CCNE1 degrader-2 (compound 150A) induces the degradation of CCNE1 in CAL51 cells (paDC50 = 7.7 nM, Dmax = 88.2 %); it also exhibits antiproliferative activity against Kuramochi ovarian cancer cells (GI50 = 143.0 nM, GImax = 96.8 %)[1].
CCNE1 degrader-2 exhibits dose-dependent antiproliferative activity against multiple ovarian cancer cell lines, including Kuramochi, FU‑OV‑1, OVISE, NIH:OVCAR‑3, and OVSAHO[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CCNE1 degrader-2 (3-30 mpk PO BID; 28 days) exhibits dose-dependent tumor growth inhibition at all tested doses in the HCC1569 breast cancer CDX mouse model and the OVSAHO ovarian cancer CDX mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c nude mice were subcutaneously inoculated on the right flank with 1 × 107 MKN1 cells in 0.1 mL of RPMI‑1640 and Matrigel (1:1 ratio)[1]
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Dosage:30 mpk
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Administration:Oral (PO) administration; twice daily; for 21 days
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Result:Significantly inhibited tumor growth and reduced CCNE1 protein levels.
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Animal Model:Female NOD/SCID mice were subcutaneously inoculated on the right flank with 2 × 106 HCC1569 cells in 0.1 mL of PBS and Matrigel (1:1 ratio)[1]
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Dosage:3, 10, 30 mpk
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Administration:Oral (PO) administration; twice daily; for 28 days
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Result:Exhibited dose‑dependent tumor growth inhibition.
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Animal Model:Female NOD/SCID mice were implanted with one estradiol pellet (0.36 mg/60‑day release) in the left flank two days prior to cell inoculation, then subcutaneously inoculated on the right flank with 1×107 OVSAHO cells in 0.2 mL of RPMI‑1640 and Matrigel (1:1 ratio)[1]
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Dosage:3, 10, 30 mpk
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Administration:Oral (PO) administration; twice daily; for 28 days
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Result:Significantly suppressed tumor growth.
Chemical Information
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CAS No. 3133169-21-5
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Molecular Weight 542.56
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Formula C30H27FN4O5
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SMILES
O=C1N(C2C(NC(CC2)=O)=O)CC3=CC=C(N4[C@H](CN(C5=CC=C(C=C5)OC6=CC=C(C=C6)F)C(C4)=O)C)C=C31
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CCNE1 degrader-2 Related Classifications
HY-189497 Related Classifications
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