A-83-01, an inhibitor of TGF-β type I receptor, increased the expression of Myf5 and MyoD, and enhanced myotube formation.The targeting efficacy of single intravenous injections of F-SL combined with A-83-01 was evaluated by measurement of the biodistribution and the antitumor effect in mice bearing murine lung carcinoma M109. A-83-01 temporarily changed the tumor vasculature around 3 h post injection. A-83-01 induced 1.7-fold higher compound accumulation of F-SL in the tumor than liposome alone at 24 h post injection.
|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||50 mM in DMSO|
|Source||Breast Cancer Res Treat (2017). Figure 6. A 83-01|
|Cell Lines||SKBR3 cells|
|Incubation Time||16 h|
|Results||As shown in Fig. 6c that A83-01 alone reduced approximately 17% cell migration of JIMT1 and trastuzumab alone inhibited 20% cell migration, while in combination of A83-01 and trastuzumab synergistically inhibited JIMT1 cell migration up to 90%.|
Role of endogenous TGF-β family in myogenic differentiation of C2C12 cells.
Furutani Y,et.al. J Cell Biochem. 2011 Feb;614-24. PMID: 21268083.
Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor.
Taniguchi Y,et.al. Cancer Sci. 2010 Oct;2207-13. PMID: 20608940.
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