[CAS NO. 778277-15-9] GNF-5
PRODUCTS SPECIFICATIONS [778277-15-9]
DESCRIPTION [778277-15-9]
Overview
| MDL | MFCD16877246 |
|---|---|
| Molecular Weight | 418.37 |
| Molecular Formula | C20H17F3N4O3 |
| SMILES | FC(F)(F)OC(C=C1)=CC=C1NC2=NC=NC(C3=CC=CC(C(NCCO)=O)=C3)=C2 |
3 Publications Citing Use of MCE
Summary
GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC 50 value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer [1] [2] .
IC50 & Target
IC50: 0.22 µM (Abl) [1]
In Vitro
GNF-5 has inhibition of wild-type Abl with an IC 50 value of 0.22 µM but no inhibition for myristate site mutant E505K (IC 50 ＞10 µM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | wild type and mutant Bcr-Abl expressing Ba/F3 cells |
| Concentration: | 0.2, 0.8 and 1.6 μM |
| Incubation Time: | 48 h |
| Result: | Inhibited wild-type Abl in a non-ATP competitive fashion. |
In Vivo
GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters
[1]
.
GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses
[1]
.
GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Balb/c mice [1] | ||||||||||||||||
| Dosage: | 5 mg/kg, 20 mg/kg | ||||||||||||||||
| Administration: | 5 mg/kg intravenously or 20 mg/kg orally | ||||||||||||||||
| Result: |
|
| Animal Model: | p210 xenograft model [1] |
| Dosage: | 50 or 100 mg/kg |
| Administration: | oral, twice daily, for 7 days |
| Result: | Could normalize blood counts and spleen size. |
| Animal Model: | Bone marrow transduction/transplantation model [1] |
| Dosage: | 75 mg/kg |
| Administration: | twice daily |
| Result: |
Showed no significant response (alone).
Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib. |
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 : ≥ 49 mg/mL ( 117.12 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3902 mL | 11.9511 mL | 23.9023 mL |
| 5 mM | 0.4780 mL | 2.3902 mL | 4.7805 mL |
| 10 mM | 0.2390 mL | 1.1951 mL | 2.3902 mL |
References
