| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PLX647 dihydrochloride has an IC50 of 92 nM and potently suppresses BCR-FMS cell growth in vitro. An IC50 of 180 nM for PLX647 dihydrochloride similarly indicates that a related Ba/F3 cell line expressing BCR-KIT is very susceptible to the drug. 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 dihydrochloride suppresses endogenous FMS and KIT[1]. FLT3-ITD-expressing MV4-11 cells are potently inhibited from growing by PLX647 dihydrochloride (IC50=110 nM). The growth of Ba/F3 cells expressing BCR-KDR is only slightly inhibited by PLX647 dihydrochloride (IC50=5 μM). The osteoclast differentiation is inhibited by PLX647 dihydrochloride, with an IC50 of 0.17 μM[1].
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|---|---|
| ln Vivo |
In UUO kidney and blood monocytes, PLX647 dihydrochloride (40 mg/kg; po; twice daily for 7 days) decreases macrophage accumulation[1]. Male Swiss Webster mice exposed to 40 mg/kg of PLX647 dihydrochloride po decrease the release of IL-6 and TNF-α after exposure to LPS[1]. On collagen-induced arthritis, PLX647 dihydrochloride (20–80 mg/kg; po; once or twice daily from 27–41 days) exhibits effects[1]. Bone osteolysis and TRAP5b immunostaining are significantly inhibited by PLX647 dihydrochloride (30 mg/kg). The ability of PLX647 dihydrochloride (30 mg/kg BID) to stop tumor cells from damaging bone[1].
|
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (mouse unilateral ureter obstruction model)[1]
Doses: 40 mg/kg Route of Administration: Po; twice (two times) daily for 7 days Experimental Results: Resulted in reduction in the levels of F4/80+ macrophages by 77%. Animal/Disease Models: 7-9 wk old Male DBA/1J mice ( Mouse collagen-induced arthritis model)[1] Doses: 20 mg/kg, 80 mg/kg Route of Administration: Po; daily (20 mg/kg) from 27-41 days, twice (two times) daily (80 mg/kg) from 27-41 days Experimental Results: 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. |
| References |
| Molecular Formula |
C21H19CL2F3N4
|
|---|---|
| Molecular Weight |
455.30
|
| Exact Mass |
454.093
|
| CAS # |
1779796-38-1
|
| Related CAS # |
PLX647;873786-09-5
|
| PubChem CID |
78243730
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
30
|
| Complexity |
493
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(C1=CN=C(NCC2C=CC(C(F)(F)F)=CC=2)C=C1)C1=CNC2=NC=CC=C12.Cl
|
| InChi Key |
MVMKWLRKACAUTB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H17F3N4.2ClH/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);2*1H
|
| Chemical Name |
5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]pyridin-2-amine;dihydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1964 mL | 10.9818 mL | 21.9635 mL | |
| 5 mM | 0.4393 mL | 2.1964 mL | 4.3927 mL | |
| 10 mM | 0.2196 mL | 1.0982 mL | 2.1964 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.
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