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PLX5622

Product Name
PLX5622
CAS No.
1303420-67-8
Chemical Name
PLX5622
Synonyms
PLX5622;PLX 5622;PLX-5622;PLX5622 USP/EP/BP;PLX5622 (free base);PLX5622, 10 mM in DMSO;6-Fluoro-N-[(5-fluoro-2-methoxy-3-pyridyl)methyl]-5-[(5-methyl-7-azaindole-3-yl)methyl]pyridin-2-amine;5-Fluoro-N-[6-fluoro-5-[(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-2-methoxy-3-pyridinemethanamine;6-FLUORO-N-((5-FLUORO-2-METHOXYPYRIDIN-3-YL)METHYL)-5-((5-METHYL-1H-PYRROLO[2,3-B]PYRIDIN-3-YL)METHYL)PYRIDIN-2-AMINE;3-Pyridinemethanamine, 5-fluoro-N-[6-fluoro-5-[(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-2-methoxy-;PLX5622,PLX 5622,Inhibitor,CSF-1 receptor,microglial,CSF1R,orally,pathology,inhibit,c-Fms,penetrant,preceding,brain,colony stimulating factor 1 receptor,CSF-1R,elimination
CBNumber
CB15476531
Molecular Formula
C21H19F2N5O
Formula Weight
395.41
MOL File
1303420-67-8.mol
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PLX5622 Property

Density 
1.364±0.06 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
Soluble in DMSO (>25 mg/ml)
pka
13?+-.0.40(Predicted)
form 
solid
color 
Pale yellow
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChI
InChI=1S/C21H19F2N5O/c1-12-5-17-14(9-26-20(17)25-8-12)6-13-3-4-18(28-19(13)23)24-10-15-7-16(22)11-27-21(15)29-2/h3-5,7-9,11H,6,10H2,1-2H3,(H,24,28)(H,25,26)
InChIKey
NSMOZFXKTHCPTQ-UHFFFAOYSA-N
SMILES
C1(OC)=NC=C(F)C=C1CNC1=NC(F)=C(CC2C3=CC(C)=CN=C3NC=2)C=C1
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
28927
Product name
PLX5622
Packaging
1mg
Price
$26
Updated
2024/03/01
Cayman Chemical
Product number
28927
Product name
PLX5622
Packaging
25mg
Price
$275
Updated
2024/03/01
Cayman Chemical
Product number
28927
Product name
PLX5622
Packaging
5mg
Price
$106
Updated
2024/03/01
Cayman Chemical
Product number
28927
Product name
PLX5622
Packaging
10mg
Price
$172
Updated
2024/03/01
ChemScene
Product number
CS-0077157
Product name
PLX5622
Purity
99.86%
Packaging
5mg
Price
$120
Updated
2021/12/16
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PLX5622 Chemical Properties,Usage,Production

Description

PLX5622 (1303420-67-8) is a highly selective (>20 fold over KIT and FLT3, >60 fold over 200 other kinases) and brain-penetrant inhibitor of colony-stimulating factor 1 receptor (CSF1R; IC50 = 16 nM).1 It prevented plaque formation in 5xFAD1 and 3xTg2 mouse models of Alzheimer’s disease via elimination of microglia in a CSF1R-dependent manner.? PLX5622 showed efficacy in a mouse neuropathic pain model via reduction of CD86+ macrophages resulting in reduced expression of pro-inflammatory cytokines.3 It also was able to ameliorate peripheral neuropathy in aging mice.4 PLX5622 displayed neuroprotective effects during the chronic phase of a traumatic brain injury mouse model.5? PLX5622 has also been shown to affect myeloid and lymphoid compartments, indicating that its affects are not limited to microglia and include peripheral immune cells.6

Uses

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 cells elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals[1][2].

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]

SpeciesIVPO (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
Mouse1.9215,5002.10.342.645215,00026,30059%
Rat (male)1.132,6307.71.22.34599,60012,00095%
Rat (female)1.135,1103.71.03.945181,00015,60089%
Dog1.006,2303.02.3154596,5003,63034%
Monkey1.352,100111.62.2NDNDNDND

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.

References

[1] ELIZABETH SPANGENBERG. Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer’s disease model.[J]. ACS Combinatorial Science, 2019: 3758. DOI:10.1038/s41467-019-11674-z
[2] NABIL N DAGHER. Colony-stimulating factor 1 receptor inhibition prevents microglial plaque association and improves cognition in 3xTg-AD mice.[J]. Journal of Neuroinflammation, 2015: 139. DOI:10.1186/s12974-015-0366-9
[3] SEUNGHWAN LEE. Targeting macrophage and microglia activation with colony stimulating factor 1 receptor inhibitor is an effective strategy to treat injury-triggered neuropathic pain.[J]. Molecular Pain, 2018, 14: 1744806918764979. DOI:10.1177/1744806918764979
[4] XIDI YUAN. Macrophage Depletion Ameliorates Peripheral Neuropathy in Aging Mice.[J]. Journal of Neuroscience, 2018, 38 19: 4610-4620. DOI:10.1523/jneurosci.3030-17.2018
[5] REBECCA J HENRY. Microglial Depletion with CSF1R Inhibitor During Chronic Phase of Experimental Traumatic Brain Injury Reduces Neurodegeneration and Neurological Deficits.[J]. Journal of Neuroscience, 2020: 2960-2974. DOI:10.1523/jneurosci.2402-19.2020
[6] FENGYANG LEI. CSF1R inhibition by a small-molecule inhibitor is not microglia specific; affecting hematopoiesis and the function of macrophages.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2020: 23336-23338. DOI:10.1073/pnas.1922788117

PLX5622 Preparation Products And Raw materials

Raw materials

Preparation Products

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PLX5622 Suppliers

China 115 India 1 United States 8 Global 124
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
Changzhou Borl Biotechnology Co.,LTD
Tel
13606124132;13656121842
Email
luyan0021@163.com
Country
China
ProdList
235
Advantage
58
Chuzhou KeMail Chemical Technology Co., Ltd
Tel
0550-5196001 15000891977
Fax
0550-5196001
Email
wj520wjxby@126.com
Country
China
ProdList
1944
Advantage
55
Olix (Shanghai) Pharmaceutical Technology Co., Ltd
Tel
17316404525 17316404525
Email
209533805@qq.com
Country
China
ProdList
9766
Advantage
58
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
Advantage
62
Changsha Fuzhen Biotechnology Co.，LTD
Tel
0731-13823398 15111215862
Email
313359644@qq.com
Country
China
ProdList
4161
Advantage
58
Hunan Huayi Zhide Pharmaceutical Technology Co., Ltd.
Tel
17752881701
Email
190060276@qq.com
Country
China
ProdList
170
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58
Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2989
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58
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Fax
020-39119999
Email
isunpharm@qq.com
Country
China
ProdList
4720
Advantage
55
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View Lastest Price from PLX5622 manufacturers

Zibo Hangyu Biotechnology Development Co., Ltd
Product
PLX5622 1303420-67-8
Price
US $150.00-150.00/KG
Min. Order
1KG
Purity
0.99
Supply Ability
20 tons
Release date
2023-10-07
Shanghai Qianyi New Material Co., Ltd.
Product
PLX5622 1303420-67-8
Price
US $2900.00-22118.00/g
Min. Order
1g
Purity
99%
Supply Ability
5000
Release date
2023-05-22
Dideu Industries Group Limited
Product
PLX5622 1303420-67-8
Price
US $1.10/g
Min. Order
1g
Purity
99.9%
Supply Ability
100 Tons min
Release date
2021-08-17

1303420-67-8, PLX5622Related Search:

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  • PLX5622
  • PLX 5622;PLX-5622
  • 3-Pyridinemethanamine, 5-fluoro-N-[6-fluoro-5-[(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-2-methoxy-
  • 5-Fluoro-N-[6-fluoro-5-[(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-2-methoxy-3-pyridinemethanamine
  • PLX5622 USP/EP/BP
  • 6-FLUORO-N-((5-FLUORO-2-METHOXYPYRIDIN-3-YL)METHYL)-5-((5-METHYL-1H-PYRROLO[2,3-B]PYRIDIN-3-YL)METHYL)PYRIDIN-2-AMINE
  • PLX5622,PLX 5622,Inhibitor,CSF-1 receptor,microglial,CSF1R,orally,pathology,inhibit,c-Fms,penetrant,preceding,brain,colony stimulating factor 1 receptor,CSF-1R,elimination
  • 6-Fluoro-N-[(5-fluoro-2-methoxy-3-pyridyl)methyl]-5-[(5-methyl-7-azaindole-3-yl)methyl]pyridin-2-amine
  • PLX5622 (free base)
  • PLX5622, 10 mM in DMSO
  • 1303420-67-8
  • API