| PLX647dual inhibitor of FMS and KIT kinases |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 99.21%
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| Cas No. | 873786-09-5 | SDF | Download SDF |
| Chemical Name | (E)-N-(5-((1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)pyridin-2(1H)-ylidene)-1-(4-(trifluoromethyl)phenyl)methanamine | ||
| Canonical SMILES | FC(F)(F)C1=CC=C(C/N=C2C=CC(CC3=CNC4=C3C=CC=N4)=CN2)C=C1 | ||
| Formula | C21H17F3N4 | M.Wt | 382.38 |
| Solubility | ≥19.1mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
PLX647 is a potent and specific dual inhibitor of FMS and KIT kinases with IC50 values of 28 and 16 nM, respectively [1].
McDonough feline sarcoma viral (v-fms) oncogene homolog (FMS, also known as CSF1R) is a member of the platelet-derived growth factor receptor (PDGFR) family. Macrophage colony-stimulating factor (M-CSF or CSF-1) and interleukin 34 are two known FMS ligands. FMS plays important roles in regulating the survival, proliferation, and differentiation of monocyte/macrophage lineages. The stem cell factor (SCF) receptor v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog (KIT) is also a member of the PDGFR family. Mutational activation of KIT occurs in many cancers [1].
PLX647 is a potent and specific dual inhibitor of FMS and KIT kinases. PLX647 showed aqueous solubility of 14 μM. PLX647 bound to the autoinhibited state of the KIT kinase with the juxtamembrane domain and prevented the activation loop from adopting the DFG-in conformation. In Ba/F3 cells expressing breakpoint cluster region activated kinase (BCR)-FMS and BCR-KIT, PLX647 inhibited cell proliferation with IC50 values of 0.092 and 0.18 μM. Also, PLX647 inhibited osteoclast differentiation with IC50 value of 0.17 μM [1].
In mice, PLX647 (40 mg/kg) significantly reduced LPS-induced TNF-α and IL-6 release by 85% and 75%, respectively. In an acute renal inflammation mouse model, PLX647 (40 mg/kg twice daily) reduced the levels of F4/80+ macrophages by 77% [1].
Reference:[1]. Zhang C, Ibrahim PN, Zhang J, et al. Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A, 2013, 110(14): 5689-5694.
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个人感觉这个就是厂家的一个噱头，，，听说有人已经在无抗猪肉中发现抗药性细菌，不知是真是假，不过要买的话一定要去信誉的地方。
以上回答，希望对你有用。
