KX2-391 is a synthetic, orally bioavailable small molecule and non-ATP competitive Src tyrosine kinase signaling inhibitor with an IC50 of average 72 nM. KX2-391 has potential antineoplastic activity. Src kinase inhibitor KX2-391 specifically binds to the peptide substrate binding site of Src kinase. In addition, KX2-391 also inhibits microtubule polymerization. Preclinical studies have suggested that KX2-391 is able to prevent the proliferation and metastasis of prostate cancer cell lines in mouse xenografts. KX2-391 phase I clinical trials have been completed.
|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 60 mg/mL|
|Related Src-bcr-Abl Products|
GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.
Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.
Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
Dasatinib(BMS-354825) hydrochloride is a potent and dual Abl/ Src inhibitor IC50 of ＜1 nM/0.8 nM respectively; also inhibit c-Kit (WT)/c-Kit (D816V) with IC50 of 79 nM/37 nM.
MCB-613 is a potent steroid receptor coactivator (SRC) stimulator.
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