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CGP77675

Cat. No. M8287
CGP77675 Structure
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Biological Activity

CGP77675 is a potent Src kinase inhibitor. CGP77675 is selective toward other protein kinases including Cdc2 (>500-fold), epidermal growth factor (EGF) receptor (7.5-fold), vascular endothelial growth factor receptor (>50-fold), and for v-Abl (15-fold) and focal adhesion kinase (Fak) (>25-fold).

Chemical Information
Molecular Weight 443.54
Formula C26H29N5O2
CAS Number 234772-64-6
Solubility (25°C) DMSO: ≥10 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] Sebla Dincer, et al. Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors

[2] Nadia Rucci, et al. Inhibition of protein kinase c-Src as a therapeutic approach for cancer and bone metastases

[3] Qiwei Zhang, et al. Inhibition of Src kinases combined with CD40 ligand blockade prolongs murine cardiac allograft survival

[4] Travis C Jackson, et al. Modulation of cyclic AMP production by signal transduction pathways in preglomerular microvessels and microvascular smooth muscle cells

[5] M Missbach, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellular substrates and reduces bone resorption in vitro and in rodent models in vivo

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Keywords: CGP77675 supplier, inhibitors, activators

 
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