[CAS NO. 1190094-64-4] CP-609754
PRODUCTS SPECIFICATIONS [1190094-64-4]
DESCRIPTION [1190094-64-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 479.96 |
| Molecular Formula | C29H22ClN3O2 |
| SMILES | O=C1N(C)C2=C(C=C([C@](O)(C3=CC=C(Cl)C=C3)C4=CN=CN4C)C=C2)C(C5=CC=CC(C#C)=C5)=C1 |
Summary
In Vitro
CP-609754 (CP-609,754) is a reversible inhibitor of farnesyltransferase with a slow on/off rate. CP-609,754 inhibits farnesylation (IC
50
=1.72 ng/mL) of mutant H-Ras in 3T3 H-ras (61L)-transfected cell lines with SDS-PAGE analysis of [
35
S]methionine-labeled material
[1]
.
CP-609754 is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI. CP-609754 interacts with the farnesyltransferase-farnesyl PPI complex and competes for the binding of the Ras protein. CP-609754 selectively inhibits farnesylation of both H- and K-Ras proteins in 3T3 transfectants
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CP-609754 (CP-609,754) has antitumor activity against 3T3 H-ras (61L) tumors in vivo
[1]
.
With twice daily oral dosing of CP-609754, tumor regression is achieved with a dose of 100 mg/kg; the ED
50
for tumor growth inhibition is 28 mg/kg
[1]
.
With continuous i.p. infusion of CP-609754, tumor growth is inhibited by >50%, and tumor farnesyltransferase activity inhibited by >30% in mice in which the plasma concentration of CP-609754 is maintained above 118 ng/mL
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01013610 | Link Medicine Corporation |
Mild Alzheimer´s Disease
|
November 2009 | Phase 1 |
| NCT00903253 | Link Medicine Corporation |
Healthy Elderly Volunteers
|
May 2009 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 208.35 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0835 mL | 10.4175 mL | 20.8351 mL |
| 5 mM | 0.4167 mL | 2.0835 mL | 4.1670 mL |
| 10 mM | 0.2084 mL | 1.0418 mL | 2.0835 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution