Cyclin A/B RxL-IN-1
Cyclin A/B RxL-IN-1 is a inhibitor targeting the Cyclin A/B RxL interaction at the hydrophobic patch (HP). Cyclin A/B RxL-IN-1 inhibits Cyclin A with an IC50 of 0.12 μM. Cyclin A/B RxL-IN-1 demonstrates antitumor efficacy in mouse cell line-derived xenograft (CDX) models. CDK-IN-19 can be used for the study of E2F-driven cancers such as small-cell lung cancer (SCLC).
For research use only. We do not sell to patients.
- CAS No.: 3036231-62-3
- Formula: C46H63Cl2F4N7O7
- Molecular Weight:972.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Cyclin A/B RxL-IN-1 (Compound 34) (5 days) inhibits proliferation of RB1/E2F-dysregulated small-cell lung cancer (SCLC) cells, with GI50 of 0.016 μM in NCI-H69 cells and 0.048 μM in NCI-H1048 cells[1].
Cyclin A/B RxL-IN-1 exhibits selective binding affinity to Cyclin A/B, with Cyclin A FP2 IC50 of 0.079 μM, and Cyclin E FP2 IC50 of 0.958 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cyclin A/B RxL-IN-1 (100 mg/kg, i.p., once daily, 18 days) demonstrates potent antitumor activity in NCI-H69 SCLC xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCI-H1048 cells (3 × 106 in 100 μL mixture of HITES media and Matrigel at 1:1 ratio) were subcutaneously implanted into the flanks of 6-8-week-old female BALB/c nude mice[1]
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Dosage:50, 100 mg/kg
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Administration:i.p., once daily, 14 days
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Result:Achieved tumor growth inhibition.
Showed no significant changes in body weight.
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Animal Model:NCI-H69 cells (5 × 106 in 100 μL mixture of serum-free RPMI-1640 media and ECM gel at 1:1 ratio) were subcutaneously implanted into the flanks of 7-8-week-old female Nude mice[1]
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Dosage:100 mg/kg
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Administration:i.p., once daily, 18 days
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Result:Achieved tumor growth inhibition.
Chemical Information
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CAS No. 3036231-62-3
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Molecular Weight 972.93
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Formula C46H63Cl2F4N7O7
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SMILES
CC(C[C@@H]1NC([C@H](CCCCNC(C(C)(NC([C@@H](N(C1=O)C)CC2=CC(Cl)=CC=C2Cl)=O)C)=O)N(C([C@H](C3CC3)NC([C@@H]4C[C@H](CN4C(C5(CC6(C5)CCC6)C(F)(F)F)=O)F)=O)=O)C)=O)C
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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)
Cyclin A/B RxL-IN-1 Related Classifications
HY-175729 Related Classifications
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