Brepocitinib

SKU: orb1296275

Description

Brepocitinib

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	1883299-62-4
MW	389.4
Purity	98.00%
Formula	C₁₈H₂₁F₂N₇O
SMILES	C(=O)(N1C2CN(CC1CC2)C3=NC(NC=4C=NN(C)C4)=NC=C3)[C@H]5C(F)(F)C5
Target	JAK,Tyrosine Kinases
Solubility	H2O:Insoluble;DMSO:75 mg/mL (192.6 mM);Ethanol:75 mg/mL (192.6 mM)

Bioactivity

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Target IC50	JAK1:17 nM (cell free)\|JAK2:77 nM (cell free)\|TYK2: 23 nM (cell free)\|JAK3:6.9 μM
In Vivo	PF-06700841 (3-30 mg/kg; p.o; for 7 consecutive days; f Male Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner the plasma concentration in animals dosed with PF-06700841 at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM. Read more...
In Vitro	PF-06700841 inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood IC50 : 65/120 nM). PF-06700841 inhibit the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency IC50 : 238/204 nM). PF-06700841 also has good potency against IL6/pStat1 in the CD3+ cellular subset IC50 81 nM), but lower Inhibition of IL6/pSTAT3, again in the CD3+ cellular subset IC50 641 nM). PF-06700841 inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells IC50 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by PF-06700841 IC50 : 305 nM/86 nM). Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Brepocitinib, Inhibitor, Janus kinase, inhibit, JAK1, JAK2, JAK3, JAK, PF-06700841, PF06700841, PF 06700841, Tyk2, Tyrosine Kinases, TyrosineKinases

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Compound Identifiers

PubChem CID

135087198 ↗

Key Properties

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No computed properties available.

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Purity:	99.82%
CAS Number:	2140301-96-6
MW:	561.6
Formula:	C₂₅H₂₉F₂N₇O₄S

Brepocitinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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