TL02-59 is a selective, orally active Src-family kinase Fgr inhibitor with IC50 of 0.03 nM, it also inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency. TL02-59 induces growth arrest in primary AML bone marrow samples.
In vivo, TL02-59 (1 and 10 mg/kg; oral; three weeks) completely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML.
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 90 mg/mL|
|Related Src-bcr-Abl Products|
1NM-PP1 is a cell-permeable and potent Src family kinases inhibitor with IC50 values of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively.
CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase.
Flumatinib mesylate is a selective inhibitor of BCR-ABL/PDGFR/c-Kit with IC50s of 1.2 nM, 307.6 nM and 2662 nM, respectively.
Asciminib, also known as ABL001, is a potent allosteric inhibitor of BCR-ABL, with a Kd value of 0.5-0.8 nM.
TG-100572 hydrochloride is a potent and selective multi-targeted VEGFR2/Src kinase inhibitor.
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