[CAS NO. 778277-15-9] GNF-5
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PRODUCTS SPECIFICATIONS [778277-15-9]
Store
Catalog
SLK-S7526
Brand
Selleck
CAS
778277-15-9
DESCRIPTION [778277-15-9]
Overview
| MDL | MFCD16877246 |
|---|---|
| Molecular Weight | 418.37 |
| Molecular Formula | C20H17F3N4O3 |
| SMILES | O=C(NCCO)C1=CC=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=C1 |
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 | 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 |
| 50 mM | 0.0478 mL | 0.2390 mL | 0.4780 mL |
Description
GNF-5 is a selective and allosteric inhibitor with of 220 nM.
Targets
| Bcr-Abl [1] |
| 220 nM |
In vitro
GNF-5, when used in combination with imatinib or nilotinib, suppresses the emergence of resistance mutations in vitro, and displays additive inhibitory activity in biochemical and cellular assays against Bcr-Abl T315I mutant. GNF-5 shows potent antiproliferative activity with EC50 of 430 nM and 580 nM against wt-Bcr-Abl and E255K mutant Bcr-Abl transformed cells, respectively.
In vivo
GNF-5 (100 mg/kg ) displays efficacy on wild-type and T315I Bcr-Abl dependent proliferation in xenograft and bone marrow transplantation models. Moreover, a combination of GNF-5 (75 mg/kg) with nilotinib (50 mg/kg) results in improved overall survival in a T315I Bcr-Abl BMT model.
References
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