[CAS NO. 873786-09-5] PLX647
PRODUCTS SPECIFICATIONS [873786-09-5]
DESCRIPTION [873786-09-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 382.38 |
| Molecular Formula | C21H17F3N4 |
| SMILES | FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=CC=C43)C=C2)C=C1)(F)F |
Summary
In Vitro
In vitro, PLX647 potently inhibits proliferation of BCR-FMS cells, with an IC
50
of 92 nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647, with an IC
50
of 180 nM. PLX647 also inhibits endogenous FMS and KIT, as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC
50
=380 nM) and M-07e (IC
50
=230 nM), which express FMS and KIT, respectively
[1]
.
PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC
50
=110 nM). PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC
50
=5 μM). PLX647 inhibits osteoclast differentiation with an IC
50
of 0.17 μM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PLX647 (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes
[1]
.
PLX647 (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release
[1]
.
PLX647 (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis
[1]
.
PLX647 (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 (30 mg/kg BID) is able to prevent bone damage by the tumor cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male C57BL/6 mice (mouse unilateral ureter obstruction model) [1] |
| Dosage: | 40 mg/kg |
| Administration: | P.o.; twice daily for 7 days |
| Result: | Resulted in reduction in the levels of F4/80+ macrophages by 77%. |
| Animal Model: | 7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model) [1] |
| Dosage: | 20 mg/kg, 80 mg/kg |
| Administration: | P.o.; daily (20 mg/kg) from 27-41 days, twice daily (80 mg/kg) from 27-41 days |
| Result: | 20 mg/kg PLX647 had no initial effect on the development of severe arthritis. However, starting on day 33, no further development of disease severity was recorded, and a 30% inhibition of the macroscopic signs of arthritis was evident in clinical score on day 41. Mice treated with 80 mg/kg BID PLX647 initially shows delayed development of severe arthritic signs. Starting on day 33, the signs of arthritis began to decrease in this treatment group, reaching a maximum reversal of 76% on day 41. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 65.38 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6152 mL | 13.0760 mL | 26.1520 mL |
| 5 mM | 0.5230 mL | 2.6152 mL | 5.2304 mL |
| 10 mM | 0.2615 mL | 1.3076 mL | 2.6152 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution
References
- [1] Zhang C, et al. Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94.
- [2] Louvet C, et al. Tyrosine kinase inhibitors reverse type 1 diabetes in nonobese diabetic mice. Proc Natl Acad Sci U S A. 2008 Dec 2;105(48):18895-900.