1. Protein Tyrosine Kinase/RTK
  2. c-Fms
  3. PLX5622

PLX5622 

Cat. No.: HY-114153 Purity: 99.95%
Handling Instructions

PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals.

For research use only. We do not sell to patients.

PLX5622 Chemical Structure

PLX5622 Chemical Structure

CAS No. : 1303420-67-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 104 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 104 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 195 In-stock
Estimated Time of Arrival: December 31
25 mg USD 390 In-stock
Estimated Time of Arrival: December 31
50 mg USD 650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of PLX5622:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals[1][2].

IC50 & Target

IC50: 0.016 µM (CSF1R); Ki: 5.9 nM (CSF1R)[1][2]

In Vitro

PLX5622 (1-20 μM; 3 days) effectively depletes microglia without affecting oligodendrocytes or astrocytes in cerebellar slices. PLX5622 (4 μM; 3 days) causes a 30-40% reduction in NG2+ or PDGFRα+ cells, and this increased to 90-95% at 20 μM. No reduction of NG2+ or PDGFRα+ OPCs is observed in slices exposed to 1 μM or 2 μM PLX5622 despite robust (~95%) depletion of the microglial cells[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pharmacodynamics of PLX5622 in preclinical studies
PLX5622 (1200 ppm; chow; for 3 weeks or 3 days; adult C57/Bl6 wild type mice) leads to around 80% of microglia lost after 3 days of treatment and a 99% microglia loss after 3 weeks of treatment. PLX5622 (adult C57/Bl6 wild type mice aged 3 months; diet for 3 weeks) decreases microglia in cortex, striatum, cerebellum and hippocampus[4].
PLX5622 (50 mg/kg; intraperitoneal injection; once (neonatal rat) or twice (adult rat) a day; for a total of 14 days) depletes microglia by 80-90% within 3 days of treatment, which increases to > 90% by 7 days. After 14 days of PLX5622 treatment, microglia is depleted by > 96% in both neonates and adults while preserving baseline astrocyte quantity. (A single daily injection of 0.65% PLX5622 suspended in 5% dimethyl sulfoxide and 20% Kolliphor RH40 in 0.01 M PBS is sufficient for neonatal microglia depletion, adult depletion requires injections twice daily)[5].
PLX5622 (formulated in AIN-76A standard chow at 1200 mg/kg; for 28 days) leads to reduction in microglia throughout the CNS in 14-month-old 5xfAD mice[6].

Pharmacokinetics of PLX5622 in preclinical species[1]

Species IV PO (gavage)
Dose
(mg/kg)
AUC0-∞
(ng•hr/mL)
CL
(mL/min/kg)
Vss
(L/kg)
t1/2
(hr)
Dose
(mg/kg)
AUC0-∞
(ng•hr/mL)
Cmax
(ng/mL)
F
Mouse 1.92 15,500 2.1 0.34 2.6 45 215,000 26,300 59%
Rat (male) 1.13 2,630 7.7 1.2 2.3 45 99,600 12,000 95%
Rat (female) 1.13 5,110 3.7 1.0 3.9 45 181,000 15,600 89%
Dog 1.00 6,230 3.0 2.3 15 45 96,500 3,630 34%
Monkey 1.35 2,100 11 1.6 2.2 ND ND ND ND

Preparation of gavage dosing suspensions for PLX5622[1]
PLX5622 is dissolved in DMSO at a concentration that is 20x the final dosing solution. The compound stock is protected from light. A fresh stock is made each week.
The components of the diluent generally are prepared a day or more in advance because they take time to dissolve completely: a) 2% hydroxypropyl methyl cellulose (HPMC): 2.0 g powder was brought to 100 mL deionized water; b) 25% Polysorbate 80 (PS80): 25 g was brought to 100 mL deionized water. To make 100 mL diluent, add 25 mL of 2% HPMC stock (0.5% final) and 4 mL of 25% PS80 stock (1% final) to 71 mL deionized water to have final 100 mL. Final composition after mixing with compound: 0.5% HPMC, 1% PS80, 5% DMSO.
On each dosing day, the compound stock is diluted 20-fold as follows: 19 volumes of diluent are measured into the tube, and 1 volume of the 20x compound/DMSO stock is added. The cap is closed and the content of the tube is mixed by inversion and placed in a sonicating water bath to make a uniform suspension.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

395.41

Formula

C21H19F2N5O

CAS No.
SMILES

COC1=NC=C(F)C=C1CNC2=NC(F)=C(CC3=CNC4=NC=C(C)C=C43)C=C2

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
In Vitro: 

DMSO : 25 mg/mL (63.23 mM; ultrasonic and warming and heat to 80°C)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5290 mL 12.6451 mL 25.2902 mL
5 mM 0.5058 mL 2.5290 mL 5.0580 mL
10 mM 0.2529 mL 1.2645 mL 2.5290 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  5% DMSO    95% (0.5% Hypromellose    1% Tween-80) (Note: To make 100 mL diluent (0.5% Hypromellose    1% Tween-80), add 25 mL of 2% Hypromellose stock and 4 mL of 25% Tween-80 stock to 71 mL ddH2O)

    Solubility: 6.5 mg/mL (16.44 mM); Suspended solution; Need ultrasonic and warming

  • 2.

    Add each solvent one by one:  5% DMSO    95% (20% Ethoxylated hydrogenated castor oil in saline)

    Solubility: 5 mg/mL (12.65 mM); Clear solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.12 mg/mL (7.89 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution

  • 5.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 99.95%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PLX5622
Cat. No.:
HY-114153
Quantity:
MCE Japan Authorized Agent: