[CAS NO. 839706-07-9] GNF-7
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PRODUCTS SPECIFICATIONS [839706-07-9]
Store
Catalog
SLK-S8140
Brand
Selleck
CAS
839706-07-9
DESCRIPTION [839706-07-9]
Overview
| MDL | MFCD18251569 |
|---|---|
| Molecular Weight | 547.53 |
| Molecular Formula | C28H24F3N7O2 |
| SMILES | O=C(NC1=CC=C(C)C(N2CC3=CN=C(NC4=CC=C(C)N=C4)N=C3N(C)C2=O)=C1)C5=CC=CC(C(F)(F)F)=C5 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8264 mL | 9.1319 mL | 18.2638 mL |
| 5 mM | 0.3653 mL | 1.8264 mL | 3.6528 mL |
| 10 mM | 0.1826 mL | 0.9132 mL | 1.8264 mL |
| 50 mM | - | - | - |
Description
GNF-7 is a potent type-II kinase inhibitor with of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively.
In vitro
GNF-7 shows potent antiproliferative activity against wild-type and mutant Bcr-Abl Ba/F3 cells with IC50 less than 11 nM. In human colon cancer cells (Colo205 and SW620), GNF-7 also displays excellent growth inhibitory activity with IC50 of 5 nM and 1 nM, respectively. GNF-7, potently and selectively inhibits NRAS-dependent acute myelogenous leukemia and acute lymphoblastic leukemia cells through combined inhibition of ACK1/AKT and GCK.
In vivo
GNF-7 exhibits excellent pharmacokinetic parameters in mice. In a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line, GNF-7 (10 mg/kg, p.o.) effectively inhibits tumor growth. In NSG mice bearing human mutant NRAS-expressing MOLT-3-luc+ tumors, GNF-7 (15 mg/kg, p.o.) significantly decreases disease burden, prolongs overall survival, and causes strong suppression of phospho-AKT and phospho-RPS6.
References
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