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PF-06700841

Cat. No. M10437
PF-06700841 Structure
Synonym:

PF-06700841 free base; Brepocitinib

Size Price Availability Quantity
5mg USD 70  USD70 In stock
10mg USD 120  USD120 In stock
25mg USD 278  USD278 In stock
50mg USD 500  USD500 In stock
100mg USD 834  USD834 In stock
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Quality Control & Documentation
Biological Activity

PF-06700841 is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. PF-06700841 also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively. PF-06700841 has good potency against IL6/pStat1 in the CD3+ cellular subset (IC50 of 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3+ cellular subset (IC50 of 641 nM). PF-06700841 also inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (HWB IC50s of 238 and 204 nM, respectively). PF-06700841 inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50 of 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by PF-06700841 with IC50s of 305 nM and 86 nM, respectively.

In vivo, PF-06700841 (3-30 mg/kg; oral administration; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner.

Chemical Information
Molecular Weight 389.40
Formula C18H21F2N7O
CAS Number 1883299-62-4
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] James G Krueger, et al. J Am Acad Dermatol. Tyrosine kinase 2 and Janus kinase‒signal transducer and activator of transcription signaling and inhibition in plaque psoriasis

[2] Christine E Jo, et al. Int J Dermatol. TYK 2 inhibitors for the treatment of dermatologic conditions: the evolution of JAK inhibitors

[3] Seth B Forman, et al. J Invest Dermatol. TYK2/JAK1 Inhibitor PF-06700841 in Patients with Plaque Psoriasis: Phase IIa, Randomized, Double-Blind, Placebo-Controlled Trial

[4] Fathima Ferial Ismail, et al. Expert Rev Clin Pharmacol. JAK inhibition in the treatment of alopecia areata - a promising new dawn?

[5] Ana M Montilla, et al. Dermatol Ther (Heidelb). Scoping Review on the Use of Drugs Targeting JAK/STAT Pathway in Atopic Dermatitis, Vitiligo, and Alopecia Areata

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  Catalog
Abmole Inhibitor Catalog




Keywords: PF-06700841, PF-06700841 free base; Brepocitinib supplier, JAK, inhibitors, activators


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