PDEδ-IN-99
K-Ras-PDEδ-IN-1
CAS: 1841464-21-8
Molecular Formula: C25H26FN5O2
PDEδ-IN-99 - Names and Identifiers
PDEδ-IN-99 - Physico-chemical Properties
| Molecular Formula | C25H26FN5O2 |
| Molar Mass | 447.5 |
| Appearance | Solid |
| Storage Condition | Sealed in dry,Room Temperature |
| In vitro study | K-Ras-PDEδ-IN-1 exhibits an IC 50 value of 12.3 μM in PaTu8902/Panc1 CTG assay. |
| In vivo study | K-Ras-PDEδ-IN-1 (oral or intraperitonealinjection; 10 mg/kg; single dose) is in different vehicles (A=5% Tween-80, 50% NaCl, 45% H2O; B=20% DMSO, 80% PEG200; C=15% DMSO, 9.5% Cremophor EL/EtOH (1:1), 75.5 % H2O) for oral and intraperitoneal (IP) administration.whereas only very low compound levels are found in plasma after oral dosage, but significantly higher plasma concentrations are found after IP administration in vehicle A, B or C at 10 mg kg.K-Ras-PDEδ-IN-1 (intravenousinjection; 3 mg kg; single dose; 24 hours) shows a significant increase of the plasma exposure as well as the terminal half-life (t 1/2 =0.4 hours)when compares to compound 93,exhibits a t 1/2 , CO, AUC 0-tz , AUC 0.inf-obs , Cl obs , and Vss 0-inf-obs values of 4.1 hours, 2790.9 ng/ml, 1646.4 h.ng/ml, 1662.5 h.ng/ml, 1.8 L/h/kg, 5.9 l/kg. |
PDEδ-IN-99 - Reference Information
| biological activity | K-Ras-PDEδ-IN-1 is a novel and effective K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds competitively with a farnesky binding bag of PDEδ at low nanomolar Kd 8 nM. |
| target | PDE4 8.3 nM (Kd) |
| in vitro study | K-Ras-PDEδ-IN-1 exhibits an IC 50 value of 12.3 μM in PaTu8902/Panc1 CTG say. |
| in vivo study | k-ras-PDEδ-IN-1 (oral or intraperitonealinjection; 10 mg/kg; single dose) is in different vehicles (A = 5% Tween-80, 50% NaCl, 45% H2O; B = 20% DMSO, 80% PEG200; C = 15% DMSO, 9.5% Cremophor EL/EtOH (1:1), 75.5% H2O) for oral and intraperitoneal (IP) administration.whereas only very low compound levels are found in plasma after oral dosage, but significantly higher plasma concentrations are found after IP administration in vehicle a, B or c at 10 mg kg. k-ras-PDEδ-in-1 (intravenousinjection; 3 mg kg; single dose; 24 hours) shows a significant increase of the plasma exposure as well as the terminal half-life (t 1/2=0.4 hours)when compares to compound 93,exhibits a t 1/2, co, AUC 0-tz , AUC 0.inf-obs, cl obs , and Vss 0-inf-obs values of 4.1 hours, 2790.9 ng/ml, 1646.4 h ng/ml, 1662.5 h ng/ml, 1.8 l/h/kg, 5.9 l/kg. |
Last Update：2024-04-09 20:52:54
