Molecular structure of Cdk4/6 Inhibitor IV, CAS Number: 359886-84-3
Cdk4/6 Inhibitor IV (CAS 359886-84-3)
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Alternate Names:
CINK4
Application:
Cdk4/6 Inhibitor IV is a cell-permeable triaminopyrimidine compound and inhibitor of Cdk4/6
CAS Number:
359886-84-3
Purity:
>95%
Molecular Weight:
456.6
Molecular Formula:
C27H32N6O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Cdk4/6 Inhibitor IV is a cell-permeable triaminopyrimidine compound acting as a reversible and ATP-competitive inhibitor of Cdk4/6 (IC50 = 1.5 µM and 5.6 µM for Cdk4/D1 and Cdk6/D1, respectively) with selectivity over Cdk5/p35 (IC50 = 25 µM), v-abl, c-met, IGF-1R and IR (IC50 > 10 µM), Cdk2/A, Cdk2/E, Cdk4/D2, Cdk6/D2 (IC50 > 50 µM) and Cdk1/B (IC50 > 100 µM). Cdk4/6 Inhibitor IV exhibits blocking of pRb phosphorylation at Ser780 and Ser795, induce cell cycle arrest (G0/G1), and apoptosis in U2OS and MRC-5 cells at 5 - 10 µM. Furthermore, it suppresses tumor growth in a Xenograft mouse model (30 mg/kg, i.p.).
Cdk4/6 Inhibitor IV (CAS 359886-84-3) References
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- Inactivation of the Dlc1 gene cooperates with downregulation of p15INK4b and p16Ink4a, leading to neoplastic transformation and poor prognosis in human cancer. | Qian, X., et al. 2012. Cancer Res. 72: 5900-11. PMID: 23010077
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- Human epidermal growth factor receptor 4 (Her4) Suppresses p53 Protein via Targeting the MDMX-MDM2 Protein Complex: IMPLICATION OF A NOVEL MDMX SER-314 PHOSPHOSITE. | Gerarduzzi, C., et al. 2016. J Biol Chem. 291: 25937-25949. PMID: 27777309
- How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? | Jorda, R., et al. 2018. J Med Chem. 61: 9105-9120. PMID: 30234987
- Nuclear Lamin A/C Expression Is a Key Determinant of Paclitaxel Sensitivity. | Smith, ER., et al. 2021. Mol Cell Biol. 41: e0064820. PMID: 33972393
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Inhibitor of:
Cdk4, Cdk5, and Cdk6.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Cdk4/6 Inhibitor IV, 5 mg | sc-203874 | 5 mg | $265.00 |