ChemicalBook > CAS DataBase List > APILIMOD

APILIMOD

Product Name
APILIMOD
CAS No.
541550-19-0
Chemical Name
APILIMOD
Synonyms
Apimod;Sta5326;Sta-5326;Sta 5326;APILIMOD;APILIMODUM;Apilimod, >98%;ApiliMod(STA5326);Apilimod Hydrochloride;Apilimod, 10 mM in DMSO
CBNumber
CB61091430
Molecular Formula
C23H26N6O2
Formula Weight
418.49
MOL File
541550-19-0.mol
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APILIMOD Property

Boiling point:
655.1±65.0 °C(Predicted)
Density 
1.24
storage temp. 
-20°C
solubility 
Soluble in DMSO (>25 mg/ml)
pka
12.56±0.10(Predicted)
form 
solid
color 
White
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChI
InChI=1S/C23H26N6O2/c1-18-5-4-6-19(15-18)17-25-28-21-16-22(29-10-13-30-14-11-29)27-23(26-21)31-12-8-20-7-2-3-9-24-20/h2-7,9,15-17H,8,10-14H2,1H3,(H,26,27,28)
InChIKey
HSKAZIJJKRAJAV-UHFFFAOYSA-N
SMILES
C(=NNC1C=C(N2CCOCC2)N=C(OCCC2=NC=CC=C2)N=1)C1=CC=CC(C)=C1
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

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

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ChemScene
Product number
CS-2341
Product name
Apilimod
Purity
99.61%
Packaging
5mg
Price
$50
Updated
2021/12/16
ChemScene
Product number
CS-2341
Product name
Apilimod
Purity
99.61%
Packaging
10mg
Price
$80
Updated
2021/12/16
ChemScene
Product number
CS-2341
Product name
Apilimod
Purity
99.61%
Packaging
50mg
Price
$120
Updated
2021/12/16
AK Scientific
Product number
SYN5487
Product name
Apilimod
Packaging
10mg
Price
$156.92
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0004744
Product name
4'-ACETYL-BIPHENYL-4-CARBOXYLIC ACID (4-[4-(2-METHOXY-PHENYL)-PIPERAZIN-1-YL]-BUTYL)-AMIDE
Purity
95.00%
Packaging
5MG
Price
$288.2
Updated
2021/12/16
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APILIMOD Chemical Properties,Usage,Production

Description

Apilimod (541550-19-0) is a potent (IC50 = 10 nM IFN-g/LPS-stimulated human PMBC’s; IC50 = 1 nM in IFN-g/SAC-stimulated human PMBC’s) IL-12/IL-23 inhibitor downregulating both at the transcriptional level.? Suppresses Th1 but not Th2 immune response.1? Inhibition was also observed in human monocytes, monocyte-derived dendritic cells, and THP-1 cells.? Apilimod’s mechanism of action is mediation of TLR signaling via inhibition of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve; IC50 = 14 nM).2? It displayed selective cytotoxic activity in B-cell non-Hodgkin lymphoma compared with normal cells.3? Apilimod prevented infection of VSV-ZEBOV and VSV-SARS-CoV-2 (IC50 = 50 nM) as well as SARS-CoV-2 strain 2019-nCoVB/USA-1WA/2020.4

Chemical Properties

Off-White Solid

Uses

Apilimod is a small-molecule that selectively suppresses synthesis of IL-12 and IL-23. Apilimod reduces dendritic cell infiltration in psoriasis.

in vivo

Apilimod (10 mg/kg, p.o.) is effective not only when administered throughout the entire experiment, but also when administration is initiated on day 30 when disease is clearly measurable but not maximal. TA-5326 causes a significant reduction in cell number only in the Th1 model, with an average percentage of inhibition of 51%±8% relative to the vehicle control. Apilimod treatment has no effect in the Th2 setting[1]. Apilimod (5 or 20 mg/kg, p.o.) reduces the level of IL-12 p40 in serum without altering body weight in EAU mice. Oral administration of Apilimod reduces the severity of experimental autoimmune uveoretinitis (EAU) by clinical and histopathological analysis[2].

IC 50

IL-4; IL-5; IL-8; IL-12; IL-23

References

[1] YUMIKO WADA. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor.[J]. Blood, 2007, 109 3: 1156-1164. DOI:10.1182/blood-2006-04-019398
[2] XINMING CAI. PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling.[J]. Chemistry & biology, 2013, 20 7: 912-921. DOI:10.1016/j.chembiol.2013.05.010
[3] S. GAYLE. Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma.[J]. Blood, 2017, 129 13 1: 1768-1778. DOI:10.1182/blood-2016-09-736892
[4] YUAN-LIN KANG. Inhibition of PIKfyve kinase prevents infection by Zaire ebolavirus and SARS-CoV-2.[J]. bioRxiv : the preprint server for biology, 2020. DOI:10.1101/2020.04.21.053058

APILIMOD Preparation Products And Raw materials

Raw materials

Preparation Products

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APILIMOD Suppliers

Canada 1 CHINA 120 China Hong Kong 1 India 2 United States 10 Global 134
Shanghai JiYi Biotechnology Co. Ltd.
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View Lastest Price from APILIMOD manufacturers

Career Henan Chemical Co
Product
APILIMOD 541550-19-0
Price
US $1.00/KG
Min. Order
1KG
Purity
95%~99%
Supply Ability
per week 100kg
Release date
2019-09-05

541550-19-0, APILIMODRelated Search:

Aprepitant Biapenem Pidotimod Semapimod Iguratimod CIVENTICHEM CV-4057 BAF-312(SiponiMod) tasquinimod Tiprotimod Ozanimod Fingolimod hydrochloride Volasertib (BI 6727) Tapinarof NOTUMib-1 4,6-Diamino-2-pyrimidinol 2-HYDROXY-4-HYDRAZINO-PYRIMIDINE 4-AMINO-6-MORPHOLINOPYRIMIDINE APILIMOD

  • APILIMOD
  • APILIMODUM
  • (E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine
  • Sta 5326
  • Sta5326
  • Sta-5326
  • ApiliMod(STA5326)
  • 3-Methylbenzaldehyde 2-[6-(4-Morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4- pyriMidinyl]hydrazone
  • 3-Methylbenzaldehyde [6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone
  • Benzaldehyde,3-methyl-,2-[6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone
  • 4-{6-[(2E)-2-(3-Methylbenzylidene)hydrazino]-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl}morpholine
  • 4-{6-[(E)-2-[(3-methylphenyl)methylidene]hydrazin-1-yl]-2-[2-(pyridin-2-yl)ethoxy]pyrimidin-4-yl}morpholine
  • N-[(e)-(3-methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine
  • STA 5326; STA5326; STA-5326
  • Apilimod, >98%
  • 4-(6-(2-(3-Methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine
  • Benzaldehyde,3-methyl-,2-[6-(4-morpholinyl)-2-[2-(2-pyridiny...
  • 1H-Benzimidazole-1-carboxylicacid,2,3-dihydro-6-oxo-,ethylester
  • Apilimod Hydrochloride
  • Apimod
  • Apilimod, 10 mM in DMSO
  • (e)-4-(6-(2-(3-methylbenzylidene)hydrazineyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine
  • 541550-19-0
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