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CID-2011756

Cat. No. M2556

CID-2011756 Structure
Size Price Availability Quantity
5mg USD 65 In stock
10mg USD 100 In stock
50mg USD 420 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CID-2011756 is a cell-active ATP competitive and specific PKD1 inhibitor that inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells. It has pan-PKD inhibitory effects (PKD2 IC50 = 0.6±0.1; PKD3 IC50 = 0.7±0.2 uM) with similar, albeit not identical, potencies which may be expected for an ATP competitive inhibitor.Protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively). Cell permeable (EC50 = 10 μM for PKD1 inhibition).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 396.87
Formula C22H21ClN2O3
CAS Number 638156-11-3
Purity >99%
Solubility DMSO
Storage at -20°C
References

Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity.
Sharlow ER, et al. PLoS One. 2011;6(10):e25134. PMID: 21998636.

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Keywords: CID-2011756 supplier, PKD, inhibitors

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