PF06650833
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $1180 | Check With Us |
| 500mg | $1680 | Check With Us |
| 1g | $2520 | Check With Us |
: Cat #: V4562 CAS #: 1817626-54-2 Purity ≥ 98%
Description: PF06650833 is a novel, potent and selective inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4) which is used to treat autoimmune diseases such as rheumatoid arthritis, lupus, and lymphomas.
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| Molecular Weight (MW) | 361.37 |
|---|---|
| Molecular Formula | C18H20FN3O4 |
| CAS No. | 1817626-54-2 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | O=C(C1=CC2=C(C(OC[C@H]([C@H](CC)[C@@H]3F)NC3=O)=NC=C2)C=C1OC)N |
| Synonyms | Zimlovisertib; PF-06650833; PF 06650833; PF06650833; PF-6650833; PF 6650833; PF6650833, |
| Protocol | In Vitro | The kinome selectivity profile of Zimlovisertib (Compound 40) 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. The ability of Zimlovisertib to inhibit five major CYP450 enzymes is assessed using pooled human liver microsomes and probe substrates for the CYP450 enzymes. At a concentration of 3 μM of Zimlovisertib, less than 5% inhibition of CYPs 1A2, 2C8, 2C9, 2D6, and 3A4 is observed. Lactam Zimlovisertib is examined for time dependent inhibition effects on six major CYP450 enzymes (CYP1A2, 2B6, 2C8, 2C9, 2C19, and 2D6) using pooled human liver microsomes and probe substrates. At 100 μM of Zimlovisertib, no time dependent CYP inhibition is observed. The potential induction of CYP3A by Zimlovisertib is assessed using cryopreserved human hepatocytes and afforded a 4.4-fold increase in mRNA at 10 μM. Lactam Zimlovisertib is assessed in a whole cell functional VEGF2R assay (PAE-KDR cell line). No activity is observed at concentrations up to and including 30 μM. In a voltage clamp assay, Zimlovisertib inhibits hERG current by 25% at 100 μM. |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.7672 mL | 13.8362 mL | 27.6725 mL | 55.3449 mL |
| 5mM | 0.5534 mL | 2.7672 mL | 5.5345 mL | 11.0690 mL |
| 10mM | 0.2767 mL | 1.3836 mL | 2.7672 mL | 5.5345 mL |
| 20mM | 0.1384 mL | 0.6918 mL | 1.3836 mL | 2.7672 mL |
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