In vitro: HA15 induces ER stress leading to cancer cell death in vitro and overcomes BRAF inhibitor resistance in melanoma cells. In vivo: HA15 induces ER stress leading to cancer cell death and exhibits strong efficacy in xenograft mouse models with melanoma cells either sensitive or resistant to BRAF inhibitors.
|Cell lines||A375 cells|
|Preparation method||Electron microscopic images of A375 cells treated for 24 hr with HA15 displayed membrane blebs characteristic of apoptotic cells。|
|Incubation time||24 h|
|Animal models||female athymic nude mice|
|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||93 mg/mL in DMSO|
Effect of Hydroxyapatite porous characteristics on healing outcomes in rabbit posterolateral spinal fusion model.
Motomiya M, et al. Eur Spine J. 2007 Dec;16(12):2215-24. PMID: 17891422.
LY2334737 is an orally available valproic acid ester of gemcitabine, a broad-spectrum antimetabolite with antineoplastic activity.
TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120).
GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).
EXP-3174 is a potent AT1 antagonist with Kis of 0.57 and 0.67 nM for rat and human forms, respectively.
NAV-2729 is a selective ARF6 inhibitor with IC50 value of 1.0 μM.
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