RO0505124
RO0505124 is a selective CDK4 inhibitor with an IC50 of 20 nM. RO0505124 reversibly binds the ATP pocket of the kinase. RO0505124 induces G1 phase arrest in cancer cells via reduced retinoblastoma protein (Rb) phosphorylation, blocking S phase progression. RO0505124 exhibits anti-proliferative activity against various cancer cells. RO0505124 delays mitosis, induces aberrant mitosis with lagging chromosomes, driving mitotic slippage and formation of multinucleated or micronucleated cells. RO0505124 inhibits G2/M phase accumulation of survivin and borealin. RO0505124 can be used for the research of cancer.
For research use only. We do not sell to patients.
- CAS No.: 443913-79-9
- Formula: C23H25N5O3S
- Molecular Weight:451.55
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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
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CDK4 20 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COLO 205 | IC50 |
2.04 μM
Compound: Ro-0505124
|
Antiproliferative activity against human COLO205 cells assessed as inhibition of S phase after 48 hrs by MTT assay
Antiproliferative activity against human COLO205 cells assessed as inhibition of S phase after 48 hrs by MTT assay
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[PMID: 16476733] |
| HCT-116 | IC50 |
3.85 μM
Compound: Ro-0505124
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Antiproliferative activity against human HCT116 cells assessed as inhibition of S phase after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells assessed as inhibition of S phase after 48 hrs by MTT assay
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[PMID: 16476733] |
| HCT-116 | IC50 |
3.9 μM
Compound: Ro-0505124
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Cell cycle arrest in Rb-competent human HCT116 cells assessed as reduction in S phase after 24 hrs using BrdUrd staining by FACS analysis
Cell cycle arrest in Rb-competent human HCT116 cells assessed as reduction in S phase after 24 hrs using BrdUrd staining by FACS analysis
|
[PMID: 16476733] |
| MDA-MB-435 | IC50 |
3.06 μM
Compound: Ro-0505124
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Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of S phase after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of S phase after 48 hrs by MTT assay
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[PMID: 16476733] |
| MDA-MB-453 | IC50 |
1.45 μM
Compound: Ro-0505124
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Antiproliferative activity against human MDA-MB-453 assessed as inhibition of S phase cells after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-453 assessed as inhibition of S phase cells after 48 hrs by MTT assay
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[PMID: 16476733] |
| NCI-H460 | IC50 |
8.12 μM
Compound: Ro-0505124
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Antiproliferative activity against human H460a cells assessed as inhibition of S phase after 48 hrs by MTT assay
Antiproliferative activity against human H460a cells assessed as inhibition of S phase after 48 hrs by MTT assay
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[PMID: 16476733] |
| RKO | IC50 |
1.6 μM
Compound: Ro-0505124
|
Antiproliferative activity against human RKO cells assessed as inhibition of S phase after 48 hrs by MTT assay
Antiproliferative activity against human RKO cells assessed as inhibition of S phase after 48 hrs by MTT assay
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[PMID: 16476733] |
| SW480 | IC50 |
3.67 μM
Compound: Ro-0505124
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Antiproliferative activity against human SW480 cells assessed as inhibition of S phase after 48 hrs by MTT assay
Antiproliferative activity against human SW480 cells assessed as inhibition of S phase after 48 hrs by MTT assay
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[PMID: 16476733] |
RO0505124 (30 min) potently and selectively inhibits recombinant human CDK4-cyclin D with an IC50 of 20 nM, showing >100-fold selectivity over CDK1 and CDK2, and relatively high selectivity across a panel of 128 kinases[1].
RO0505124 (48 h) inhibits proliferation of multiple human cancer cell lines with IC50 values ranging from 1.45 μM to 8.12 μM after 48 h of treatment[1].
RO0505124 (3.9-18.3 μM; 4-24 h) induces a G1 phase arrest and inhibits Rb phosphorylation in asynchronous HCT-116 cells[1].
RO0505124 (2 μM; 0-24 h) delays mitotic entry, prolongs mitotic duration, and induces aberrant mitosis[1].
RO0505124 (2 μM; 3-14 h) delays the accumulation of survivin and borealin proteins during G2/M phase in HeLa cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:asynchronous HCT-116 cells
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Concentration:3.9, 6.1, 18.3 μM
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Incubation Time:4, 24 h
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Result:Reduced S phase to 50% of control levels and significantly decreased Rb phosphorylation at the IC50 concentration of 3.9 μM.
Further inhibited BrdUrd incorporation and Rb phosphorylation at higher doses.
Caused a G1 phase arrest with no reduction in G2/M phase cell proportion at higher doses.
Chemical Information
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CAS No. 443913-79-9
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Molecular Weight 451.55
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Formula C23H25N5O3S
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SMILES
O=C(C1=CC=C2OCCOC2=C1)C=3SC(=NC3N)NC4=CC=C(C=C4)N5CCN(C)CC5
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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)
RO0505124 Related Classifications
HY-118447 Related Classifications
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