Companies
MedChemExpress LLC (MCE)
Products
MedChemExpress - Model GNF-7 - ...

MedChemExpress - Model GNF-7 - 839706-07-9

GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies[1][2][3].

GNF-7

MCE China：GNF-7

Brand：MedChemExpress (MCE)

Cat. No.HY-10943

CAS：839706-07-9

Purity：99.70%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.

In Vitro：GNF-7 potently inhibits wild-type Bcr-Abl (IC50Bcr-Abl mutants such as T315I (IC50=11 nM), G250E (IC5050=10 nM), F317L (IC5050[2]. GNF-7 (1 μM; 2 hours) suppresses AKT/mTOR signaling and GCK downstream[3]. GNF-7 (1 μM; 24 hours) induces of apoptosis and cell cycle arrest in NRAS mutant cell lines[3].

In Vivo：GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model[2]. GNF-7 exhibits moderate oral bioavailability (mice 36%) and Cmax (mice 3616 nM) following oral administration (mice 20 mg/kg)[2]. GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg)[2].

IC50 & Target：IC50: 133 nM (Bcr-AblWT)[1], 61 nM (Bcr-AblT315I)[1], 25 nM (ACK1)[3], 8 nM (GCK)[3] Cellular Effect Cell Line Type Value Description References

References：

[1]. Lu X, et al. Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3458-63. [Content Brief]

[2]. Choi HG, et al. A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. J Med Chem. 2010 Aug 12;53(15):5439-48. [Content Brief]

[3]. Cho, H., et al. First SAR study for overriding NRAS mutant driven acute myeloid leukemia. Journal of Medicinal Chemistry. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。