Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Ritlecitinib (PF06651600; PF-06651600) malonate, the malonate salt of PF 06651600, is an irreversible JAK3 inhibitor with anti-inflammatory activity. It inhibits JAK3 with IC50 value of 33.1 nM, and exhibits no activity (IC50 > 10000 nM) against JAK1, JAK2, and TYK2. PF-06651600 has excellent pharmacokinetics/pharmacodynamics with low clearance, benign toxicity profile and high in vivo efficacy. As a result, PF-06651600 has been in several human clinical studies. In vivo, PF-06651600 reduces disease pathology in rat adjuvant-induced arthritis as well as in mouse autoimmune encephalomyelitis models. In September 2022, FDA has accepted for filing by Pfizer Inc the New Drug Application (NDA) for ritlecitinib to treat alopecia areata.
ln Vitro |
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ln Vivo |
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Animal Protocol |
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References |
ACS Chem Biol.2016 Dec 16;11(12):3442-3451.
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Molecular Formula |
C18H23N5O5
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Molecular Weight |
389.41
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CAS # |
2140301-97-7
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Related CAS # |
1792180-81-4;2140301-97-7 (malonate);2192215-81-7;2489392-29-0;
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SMILES |
C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=O.O=C(O)CC(O)=O
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5680 mL | 12.8399 mL | 25.6799 mL | |
5 mM | 0.5136 mL | 2.5680 mL | 5.1360 mL | |
10 mM | 0.2568 mL | 1.2840 mL | 2.5680 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
ACS Chem Biol.2016 Dec 16;11(12):3442-3451. th> |
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