WHI-P97 effectively inhibited the in vitro invasiveness of EGFR-positive human cancer cells in a concentration-dependent manner. WHI-P97 was very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 microg/kg to 50 mg/kg, and LD(10) was not reached at a 50 mg/kg dose level when administered as a single i. p. or i.v. bolus dose.
|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.
|Solubility||DMSO 10 mM|
Thrombin induces expression of cytokine-induced SH2 protein (CIS) in rat brain astrocytes: involvement of phospholipase A2, cyclooxygenase, and lipoxygenase.
Ji KA, et al. Glia. 2004 Nov 1;48(2):102-11. PMID: 15378659.
Tyrosine kinase inhibitors: a new approach for asthma.
Wong WS, et al. Biochim Biophys Acta. 2004 Mar 11;1697(1-2):53-69. PMID: 15023350.
Structure-based design of novel anticancer agents.
Uckun FM, et al. Curr Cancer Drug Targets. 2001 May;1(1):59-71. PMID: 12188892.
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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.
SAR-20347 is a potent dual inhibitor of JAK1 and TYK2 with IC50 values of 23 and 0.6 nM, respectively.
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Solcitinib is a selective Janus kinase 1 (JAK1) inhibitor, for the treatment of psoriasis, lupus, and ulcerative colitis. Targer: JAK1
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