[CAS NO. 234772-64-6] CGP77675
PRODUCTS SPECIFICATIONS [234772-64-6]
DESCRIPTION [234772-64-6]
Overview
| MDL | MFCD20039929 |
|---|---|
| Molecular Weight | 443.54 |
| Molecular Formula | C26H29N5O2 |
| SMILES | OC1CCN(CCC2=CC=C(N3C=C(C4=CC=CC(OC)=C4)C5=C(N)N=CN=C53)C=C2)CC1 |
Summary
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src ( IC 50 s of 5-20 and 40 nM, respectively), and also inhibits Src , EGFR , KDR, v-Abl, and Lck with IC 50 s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity [1] .
IC50 & Target
IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck) [1]
In Vitro
CGP77675 dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC
50
value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC
50
value of 16.7 nM. These IC
50
values are similar to the value obtained with chicken Src (20 nM)
[1]
.
CGP77675 inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC
50
of 0.8 μM
[1]
.
CGP77675 (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC
50
values 0.2, 0.5, and 5.7μM) in IC8.1 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | MC3T3-E1 cells |
| Concentration: | 0.2, 1, and 5 μM |
| Incubation Time: | 3 days |
| Result: | Did not influence cell viability for up to 3 days of treatment. |
Western Blot Analysis [1]
| Cell Line: | Src-overexpressing IC8.1 cells |
| Concentration: | 0.04, 0.2, 1, 5, and 10 μM |
| Incubation Time: | 2 hours |
| Result: | Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src. |
In Vivo
CGP77675 (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice
[1]
.
CGP77675 (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body [1] |
| Dosage: | 1, 5, and 25 mg/kg |
| Administration: | Injected s.c.; twice a day |
| Result: | Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels. |
| Animal Model: | Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf [1] |
| Dosage: | 10 and 50 mg/kg |
| Administration: | Administered orally; twice a day for 6 weeks |
| Result: | Partly prevented bone loss. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 26.0 mg/mL ( 58.62 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2546 mL | 11.2729 mL | 22.5459 mL |
| 5 mM | 0.4509 mL | 2.2546 mL | 4.5092 mL |
| 10 mM | 0.2255 mL | 1.1273 mL | 2.2546 mL |
