PF-670462 dihydrochloride | Casein kinase 1δ/ε inhibitor

CAS:
 950912-80-8
Catalog Number:
 10-4692
PF-670462 supplier | CAS 950912-80-8 | Focus Biomolecules

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5mg$70.00
25mg$255.00

PF-670462 (950912-80-8) is a potent inhibitor of casein kinase 1ε/δ (CK1ε, IC50 = 7.7 nM; CK1δ, IC50 = 14 nM).1 It is a circadian clock modifier that caused robust phase delays in rats1 and Cynomolgus monkeys2. PF-670462 caused nuclear retention of the clock protein PER resulting in period lengthening in a phase-specific manner that was dependent on CK1δ inhibition and not CK1ε.3 It improved cognitive performance and reduced amyloid load in various mouse models of Alzheimer’s disease.4-6 PF-670462 slowed the progression of and increased survival of chronic lymphocytic leukemia in mice alone and in combination with Ibrutinib.7

References/Citations:

  1. Badura et al. (2007), An Inhibitor of Casein Kinase Iε Induces Phase Delays in Circadian Rhythms under Free-Running and Entrained Conditions; J. Pharmacol. Exp. Ther. 322 730
  2. Sprouse et al. (2009), Inhibition of casein kinase I epsilon/delta produces phase shifts in the circadian rhythms of Cynomolgus monkeys; Psychopharmacology (Berl) 204 735
  3. Meng et al. (2010), Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes; Proc. Natl. Acad. Sci. USA 107 15240
  4. Adler et al. (2019), Therapeutic Targeting of Casein Kinase 1δ/ε in an Alzheimer’s Disease Mouse Model; Proteome Res. 18 3383
  5. Sundaram et al. (2019), Inhibition of casein kinase 1δ improves cognitive-affective behavior and reduces amyloid load in the APP-PS1 mouse model of Alzheimer’s Disease; Sci. Rep 13743
  6. Mahoney et al. (2021), Inhibition of casein kinase 1δ/ε improves cognitive performance in adult C57BL/6J mice; Sci. Rep. 11 4746
  7. Janovska et al. (2018), Casein kinase 1 is a therapeutic target on chronic lymphocytic leukemia; Blood 131 1206
CAS:
950912-80-8
Catalog Number:
10-4692
Activity:
Casein kinase 1δ/ε inhibitor
Chemical Names:
4-[3-Cyclohexyl-5-(4-fluorophenyl)imidazol-4-yl]pyrimidin-2-amine 2HCl
Molecular Weight:
337.40
Molecular Formula:

C19H22Cl2FN5

Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
Off-white solid
Purity:

>98% HPLC
NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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