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RGB-286638

Cat. No. M10879
RGB-286638  Structure
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Biological Activity

RGB-286638 is a potent CDK inhibitor that inhibits cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 activity,IC50 1, 2, 3, 4, 5 and 5 nM, respectively, and can inhibit GSK-3β, TAK1, Jak2 and MEK1.IC50 The values are 3, 5, 50, and 54 nM, respectively.

Chemical Information
Molecular Weight 618.55458
Formula C29H37Cl2N7O4
CAS Number 784210-87-3
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Mengna Zhang, et al. Am J Cancer Res. CDK inhibitors in cancer therapy, an overview of recent development

[2] Fatima Morales, et al. Cell Cycle. Overview of CDK9 as a target in cancer research

[3] Diane A J van der Biessen, et al. Clin Cancer Res. Phase I study of RGB-286638, a novel, multitargeted cyclin-dependent kinase inhibitor in patients with solid tumors

[4] D Cirstea, et al. Leukemia. Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs

[5] Peter de Bruijn, et al. J Pharm Biomed Anal. Validated bioanalytical method for the quantification of RGB-286638, a novel multi-targeted protein kinase inhibitor, in human plasma and urine by liquid chromatography/tandem triple-quadrupole mass spectrometry

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  Catalog
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Keywords: RGB-286638 supplier, CDK, inhibitors, activators


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