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BMS-265246

Cat. No. M2323
BMS-265246 Structure
Size Price Availability Quantity
5mg USD 135  USD135 In stock
10mg USD 235  USD235 In stock
50mg USD 780  USD780 In stock
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Quality Control & Documentation
Biological Activity

BMS-265246 is a potent and selective CDK1/CDK2 selective inhibitor for CDK1/cycB and CDK2/cycE with IC50 of 6 and 9 nM, respectively. BMS-265246 inhibits the activity of CDK4/cycD with an IC50 of 0.23 μM and prevents A2780 Cytox with an IC50 of 0.76μM. BMS-265246 exhibits CDK1 and CDK2 potency that is 25- and 11-fold more potent versus CDK1 and CDK2, respectively.

Chemical Information
Molecular Weight 345.34
Formula C18H17F2N3O2
CAS Number 582315-72-8
Solubility (25°C) DMSO 20 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] Raj N Misra, et al. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues

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  Catalog
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Keywords: BMS-265246 supplier, CDK, inhibitors, activators


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