PF-06650833
- Product Name
- PF-06650833
- CAS No.
- 1817626-54-2
- Chemical Name
- PF-06650833
- Synonyms
- CS-2457;PF06650883;PF-06650833;PF-05313261;PF-05320905;PF-05387282;Zimlovisertib;PF06650833;PF 06650833;PF06650833 >=98% (HPLC);Piraxostat Impurity 16
- CBNumber
- CB63147067
- Molecular Formula
- C18H20FN3O4
- Formula Weight
- 361.37
- MOL File
- 1817626-54-2.mol
PF-06650833 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
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.
N-Bromosuccinimide Price
- Product number
- PZ0327
- Product name
- PF06650833
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $111
- Updated
- 2025/07/31
- Product number
- 28397
- Product name
- PF-06650833
- Packaging
- 5mg
- Price
- $69
- Updated
- 2021/12/16
- Product number
- 28397
- Product name
- PF-06650833
- Packaging
- 50mg
- Price
- $449
- Updated
- 2021/12/16
- Product number
- 28397
- Product name
- PF-06650833
- Packaging
- 25mg
- Price
- $259
- Updated
- 2021/12/16
- Product number
- 28397
- Product name
- PF-06650833
- Packaging
- 10mg
- Price
- $124
- Updated
- 2021/12/16
PF-06650833 Chemical Properties,Usage,Production
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-06650833 Preparation Products And Raw materials
Raw materials
Preparation Products
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