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Formula | C20H17F3N4O3 |
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Molecular Weight | 418.37 | CAS No. | 778277-15-9 | |
Solubility (25°C)* | In vitro | DMSO | 83 mg/mL (198.38 mM) | |
Ethanol | 20 mg/mL (47.8 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM. | ||
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In vitro | GNF-5, when used in combination, suppresses the emergence of resistance mutations in vitro, and displays additive inhibitory activity in biochemical and cellular assays against Bcr-Abl T315I mutant. [1] 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. [2] |
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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) results in improved overall survival in a T315I Bcr-Abl BMT model. [1] |
Kinase Assay: |
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Data from [Data independently produced by , , Leukemia, 2017, 31(5):1096-1107]
Data from [Data independently produced by , , Oncotarget, 2017, 8(24):38717-38730]
The molecular basis of Abelson kinase regulation by its αI-helix [ Elife, 2024, 12RP92324] | PubMed: 38588001 |
Structural mechanism of a drug-binding process involving a large conformational change of the protein target [ Nat Commun, 2023, 14(1):1885] | PubMed: 37019905 |
Structural mechanism of a drug-binding process involving a large conformational change of the protein target [ Nat Commun, 2023, 14(1):1885] | PubMed: 37019905 |
Src stimulates Abl-dependent phosphorylation of the guanine exchange factor Net1A to promote its cytosolic localization and cell motility [ J Biol Chem, 2023, S0021-9258(23)01915-4] | PubMed: 37271338 |
Abl kinases can function as suppressors of tumor progression and metastasis [ Front Oncol, 2023, 13:1241056] | PubMed: 37746268 |
Abl kinases can function as suppressors of tumor progression and metastasis [ Front Oncol, 2023, 10.3389/fonc.2023.1241056] | PubMed: 37746268 |
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] | PubMed: 34997030 |
Imatinib can act as an Allosteric Activator of Abl Kinase [ J Mol Biol, 2021, 434(2):167349] | PubMed: 34774565 |
ABL1, Overexpressed in Hepatocellular Carcinomas, Regulates Expression of NOTCH1 and Promotes Development of Liver Tumors in Mice [ Gastroenterology, 2020, S0016-5085(20)30334-6] | PubMed: 32171747 |
Combating acquired resistance to MAPK inhibitors in melanoma by targeting Abl1/2-mediated reactivation of MEK/ERK/MYC signaling [ Nat Commun, 2020, 11(1):5463] | PubMed: 33122628 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.