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Delcasertib

Cat. No. M10490
Delcasertib Structure
Synonym:

KAI-9803; BMS-875944

Size Price Availability Quantity
5mg USD 620  USD620 In stock
10mg USD 900  USD900 In stock
25mg USD 1750  USD1750 In stock
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Quality Control & Documentation
Biological Activity

Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor, it could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).

Chemical Information
Molecular Weight 2880.28
Formula C120H199N45O34S2
CAS Number 949100-39-4
Solubility (25°C) DMSO ≥ 60 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] A Michael Lincoff, et al. Eur Heart J. Inhibition of delta-protein kinase C by delcasertib as an adjunct to primary percutaneous coronary intervention for acute anterior ST-segment elevation myocardial infarction: results of the PROTECTION AMI Randomized Controlled Trial

[2] Yoshihiro Miyaji, et al. Drug Metab Dispos. Distribution of KAI-9803, a novel δ-protein kinase C inhibitor, after intravenous administration to rats

[3] Eric Bates, et al. Circulation. Intracoronary KAI-9803 as an adjunct to primary percutaneous coronary intervention for acute ST-segment elevation myocardial infarction

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Keywords: Delcasertib, KAI-9803; BMS-875944 supplier, PKC, inhibitors, activators


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