TCS 21311 is selective for JAK3 over JAK1, JAK2 and TYK2 (IC50 values are 1017, 2550 and 8055 nM respectively). TCS 21311 also inhibits GSK-3β, PKCα and PKCθ (IC50 values are 3, 13 and 68 nM respectively).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.
Thoma G, et al. J Med Chem. 2011 Jan 13;54(1):284-8. PMID: 21155605.
|Related JAK Products|
Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.
WHI-P97 is a JAK3 inhibitor with an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays.
SAR-20347 is a potent dual inhibitor of JAK1 and TYK2 with IC50 values of 23 and 0.6 nM, respectively.
Itacitinib, also known as INCB39110 or INCB039110, is a potent JAK1 tyrosine kinase inhibitor.
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