Zimlovisertib (PF-06650833)

Catalog No.S8531 Batch:S853101

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Technical Data

Formula

C18H20FN3O4
Molecular Weight 361.37 CAS No. 1817626-54-2
Solubility (25°C)* In vitro DMSO 72 mg/mL (199.24 mM)
Ethanol 3 mg/mL (8.3 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Zimlovisertib (PF-06650833) is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM.
Targets
IRAK4 [1]
(Cell-free assay)
0.2 nM
In vitro

The kinome selectivity profile of PF-06650833 is assessed in a panel of 278 kinases(Invitrogen) at 200 nM inhibitor concentration using the ATP Km for each kinase. Approximately 100% inhibition is observed for IRAK4 while greater than 70% inhibition is observed for the following kinases, in order of potency: IRAK1, MNK2, LRRK2, CLK4, and CK1γ1. Lactam PF-06650833 is subsequently assessed in a whole cell functional VEGF2R assay (PAE-KDR cell line). No activity was observed at concentrations up to and including 30 µM. [1].
In vivo

PF-06650833 significantly inhibits LPS-induced TNF in a dose dependent manner. Mean exposures of PF-06650833 in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of PF-06650833 at 0.3 mg/kg, 1 mg/kg, 3 mg/kg and 30 mg/kg. The fraction unbound in rat plasma of PF-06650833 is 0.3.[1]

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Male Sprague Dawley rats

  • Dosages

    0.1 mg/kg, 1 mg/kg, 3 mg/kg, 30 mg/kg

  • Administration

    Oral

Selleck's Zimlovisertib (PF-06650833) has been cited by 6 publications

IRAK1 inhibition blocks the HIV-1 RNA mediated pro-inflammatory cytokine response from microglia [ J Gen Virol, 2023, 104(5)001858] PubMed: 37256770
A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229] PubMed: 35869064
A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229] PubMed: 35869064
Pacritinib Inhibition of IRAK1 Blocks Aberrant TLR8 Signalling by SARS-CoV-2 and HIV-1-Derived RNA [ J Innate Immun, 2022, 1-11] PubMed: 35785771
Inhibition of IRAK1/4 enhances the antitumor effect of lenvatinib in anaplastic thyroid cancer cells [ Cancer Sci, 2021, 112(11):4711-4721] PubMed: 34328666
A temperature-regulated circuit for feeding behavior [ Research Square, 2021, 10.21203/rs.3.rs-916525/v1] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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