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- Takehito Yamamoto, .et al. Chemosensitivity of Patient-Derived Cancer Stem Cells Identifies Colorectal Cancer Patients with Potential Benefit from FGFR Inhibitor Therapy, Cancers (Basel), 2020, Jul 22;12(8):E2010 PMID: 32708005
- Daniel Limonta, .et al. Fibroblast growth factor 2 enhances Zika virus infection in human fetal brain, J Infect Dis, 2019, 2019 PMID: 30799482
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Anil Kumar, .et al. Human Sertoli cells support high levels of Zika virus replication and persistence, Sci Rep, 2018, 8: 5477 PMID: 29615760
Biological Activity
BGJ398 is a potent and selective inhibitor with potential antiangiogenic and antineoplastic activities of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively).
Targets
Target | Value |
---|---|
FGFR1 | IC50: 0.9nM |
FGFR3 | IC50: 1.0nM |
FGFR2 | IC50: 1.4nM |
FGFR3(K650E) | IC50: 4.9nM |
FGFR4 | IC50: 60nM |
VEGFR2 | IC50: 0.18μM |
Lyn | IC50: 0.30μM |
Kit | IC50: 0.75μM |
YES | IC50: 1.1μM |
Fyn | IC50: 1.9μM |
Abl | IC50: 2.3μM |
LCK | IC50: 2.5μM |
In vitro (25°C) | DMSO | Warmed: 1 mg/mL (1.78 mM) | |
Water | Insoluble | ||
Ethanol | Insoluble | ||
In vivo | 1%CMC-Na | 28 mg/mL | |
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq 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. |
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 17.84 mL | 89.21 mL | 178.42 mL |
0.5 mM | 3.57 mL | 17.84 mL | 35.68 mL |
1 mM | 1.78 mL | 8.92 mL | 17.84 mL |
5 mM | 0.36 mL | 1.78 mL | 3.57 mL |
*The above data is based on the productmolecular weight 560.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Catalog Num | A11159 |
---|---|
Actions | Inhibitor |
CAS No. | 872511-34-7 |
Formula | C26H31Cl2N7O3 |
M. Wt | 560.48 |
Purity | >98% |
Synonyms | BGJ-398 |
SMILES | CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl |
Storage | Store lyophilized at -20ºC, keep desiccated. |
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