(-) -IndolacTAM V is an activator of PKC, and the Ki values of η -CrD2 (PKCγ -substituted peptide) and γ -CrD2 (PKCγ -substituted peptide) are 3.36 nM and 1.03 μM, respectively. The Kd values for C1A and C1B domains of PKC were 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), respectively. At 137 nM (β-C1B), 138 nM (γ-C1A) and 213 nM (γ-C1B), it has antitumor activity.
Molecular Weight | 301.38 |
Formula | C17H23N3O2 |
CAS Number | 90365-57-4 |
Solubility (25°C) | DMSO ≥ 40 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
[4] Zhengren Xu, et al. Org Biomol Chem. Total synthesis of (-)-indolactam V
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