Basic information Safety Supplier Related

PF-06650833

Basic information Safety Supplier Related

PF-06650833 Basic information

Product Name:
PF-06650833
Synonyms:
  • PF-06650833
  • 1-(((2S,3S,4S)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl)methoxy)-7-methoxyisoquinoline-6-carboxamide
  • 6-Isoquinolinecarboxamide,1-(((2S,3S,4S)-3-ethyl-4-fluoro-5-oxo-2-pyrrolidinyl)methoxy)-7-methoxy-
  • PF06650833;PF 06650833
  • CS-2457
  • 1-[[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxo-2-pyrrolidinyl]methoxy]-7-methoxy-6-isoquinolinecarboxamide
  • PF06650833 >=98% (HPLC)
  • PF06650883
CAS:
1817626-54-2
MF:
C18H20FN3O4
MW:
361.37
Product Categories:
  • API
Mol File:
1817626-54-2.mol
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PF-06650833 Chemical Properties

Boiling point:
621.0±55.0 °C(Predicted)
Density 
1.34±0.1 g/cm3(Predicted)
storage temp. 
room temp
solubility 
DMSO : ≥ 33 mg/mL (91.32 mM)
form 
powder
pka
13.44±0.70(Predicted)
color 
white to beige
InChIKey
JKDGKIBAOAFRPJ-ZBINZKHDSA-N
SMILES
C1(OC[C@@H]2[C@H](CC)[C@H](F)C(=O)N2)C2=C(C=C(C(N)=O)C(OC)=C2)C=CN=1
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PF-06650833 Usage And Synthesis

Uses

Zimlovisertib (PF-06650833) is a potent, selective and orally active inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4) with IC50s of 0.2 and 2.4 nM in the cell and PBMC assay, respectively. Zimlovisertib is used to treat diseases such as rheumatoid arthritis, lupus, and lymphomas[1][2].

Biochem/physiol Actions

PF06650833 has been studied for its use in the treatment of Waldenstrom macroglobulinemia, indicated by overproduction of IgM (immunoglobulin M)-producing lymphoplasmacytic cells.

in vivo

Zimlovisertib (0.3-30 mg/kg; oral administration; for 2.5 hours; male Sprague-Dawley rats) treatment significantly inhibits LPS-induced TNF-α in a dose dependent manner. Mean exposures of Zimlovisertib in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of Zimlovisertib at 0.3, 1, 3, and 30 mg/kg. The fraction unbound in rat plasma of Zimlovisertib is 0.3[1].

Animal Model:Male Sprague-Dawley rats[1]
Dosage:0.1 mg/kg, 1 mg/kg, 3 mg/kg, 30 mg/kg
Administration:Oral administration; for 2.5 hours
Result:Significantly inhibited LPS-induced TNF-α in a dose dependent manner.

IC 50

IRAK4: .2 nM (IC50)

storage

Store at -20°C

References

[1] Lee KL, et al. Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design. J Med Chem. 2017 Jul 13;60(13):5521-5542. DOI:10.1021/acs.jmedchem.7b00231
[2] Seganish WM. Inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4): a patent review (2012-2015). Expert Opin Ther Pat. 2016 Aug;26(8):917-32. DOI:10.1080/13543776.2016.1202926

PF-06650833Supplier

Dezhou LonWel Pharmaceutical Technology Co., Ltd. Gold
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13761310616
Email
39324283@qq.com
Shanghai Topbiochem Technology Co., Ltd
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021-58170097
Email
info@topbiochem.com
MedChemexpress LLC
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021-58955995
Email
sales@medchemexpress.cn
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
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