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Purity: ≥98%
PLX-647 (PLX647) is a novel, potent and highly specific dual FMS/KIT kinase inhibitor with anticancer activity. With IC50 values of 28/16 nM, it inhibits both FMS and KIt. When compared to other kinases, PLX647 exhibits high selectivity. With distinct dual FMS and KIT specificity, PLX647 belongs to a special class of kinase inhibitors.
| ln Vitro |
PLX647 has an IC50 of 92 nM and strongly suppresses BCR-FMS cell proliferation in vitro. Similarly, a corresponding Ba/F3 cell line that expresses BCR-KIT has an IC50 of 180 nM, making it highly sensitive to PLX647. Moreover, ligand-dependent cell lines that express FMS and KIT, respectively, such as M-NFS-60 (IC50=380 nM) and M-07e (IC50=230 nM), show that PLX647 inhibits endogenous FMS and KIT[1].
PLX647 inhibits FLT3-ITD-expressing MV4-11 cell growth potently (IC50=110 nM). The proliferation of Ba/F3 cells expressing BCR-KDR was minimally inhibited by PLX647 (IC50=5 μM). With an IC50 of 0.17 μM, PLX647 inhibits the differentiation of osteoclasts[1]. |
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| ln Vivo |
PLX647 (40 mg/kg; p.o.; twice daily for 7 days) decreases the accumulation of macrophages in UUO kidney and blood monocytes[1].
PLX647 (40 mg/kg; p.o.; male Swiss Webster mice) inhibits the release of TNF-α and IL-6 triggered by LPS[1]. PLX647 (20–80 mg/kg; p.o.; once or twice daily for 27–41 days) exhibits effects on arthritis caused by collagen[1]. PLX647 (30 mg/kg) causes TRAP5b immunostaining and bone osteolysis to be significantly inhibited. Tumor cell-induced bone damage can be avoided with PLX647 (30 mg/kg BID)[1]. |
| Animal Protocol |
Male C57BL/6 mice (mouse unilateral ureter obstruction model)[1]
40 mg/kg P.o.; twice daily for 7 days |
| References |
| Molecular Formula |
C21H17F3N4
|
|---|---|
| Molecular Weight |
382.381694555283
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| Exact Mass |
382.14
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| Elemental Analysis |
C, 65.96; H, 4.48; F, 14.91; N, 14.65
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| CAS # |
873786-09-5
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| Related CAS # |
PLX647 dihydrochloride;1779796-38-1
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| Appearance |
white solid powder
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| SMILES |
C1=CC2=C(NC=C2CC3=CN=C(C=C3)NCC4=CC=C(C=C4)C(F)(F)F)N=C1
|
| InChi Key |
NODCQQSEMCESEC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H17F3N4/c22-21(23,24)17-6-3-14(4-7-17)11-26-19-8-5-15(12-27-19)10-16-13-28-20-18(16)2-1-9-25-20/h1-9,12-13H,10-11H2,(H,25,28)(H,26,27)
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| Chemical Name |
5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]pyridin-2-amine
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| Synonyms |
PLX-647; PLX 647; PLX647
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~25 mg/mL (~65.4 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Scaffold-based discovery of PLX647 and structural basis of its dual-binding specificity.
PLX647 inhibits cancer bone pain and osteolysis.Proc Natl Acad Sci U S A.2013 Apr 2;110(14):5689-94. |
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 PLX647 reduces macrophage accumulation in UUO kidney and blood monocytes.Proc Natl Acad Sci U S A.2013 Apr 2;110(14):5689-94. |
 The effect of PLX647 on mouse CIA.Proc Natl Acad Sci U S A.2013 Apr 2;110(14):5689-94. |
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