GK921 showed cytotoxicity to RCC (average GI50 in eight RCC cell lines: 0.905 μM). A single treatment with GK921 almost completely reduced tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models. GK921 rescues p53 levels and consequently induces apoptosis; a concentration-dependent increase in cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels is observed.
|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: ≥ 25 mg/mL|
Discovery of a novel target for renal cell carcinoma: transglutaminase 2.
Kang JH, et al. Cell Death Dis. 2016 Apr 21;7:e2200. PMID: 27100894.
Renal cell carcinoma escapes death by p53 depletion through transglutaminase 2-chaperoned autophagy.
Kang JH, et al. Cell Death Dis. 2016 Mar 31;7:e2163. PMID: 27031960.
Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models.
Ku BM, et al. J Cancer Res Clin Oncol. 2014 May;140(5):757-67. PMID: 24610445.
Coelenterazine is the luciferin, the light-emitting molecule, used for monitoring reporter genes in BRET, ELISA and HTS techniques.
Fluorescein is a synthetic organic compound and dye.
SBI-0640756 is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex.
UKI-1 is a novel synthetic inhibitor of the urokinase-type plasminogen activator, which inhibits the invasive capacity of carcinoma cells with a Ki of 0.41 μM.
CID5721353 is a B-Cell Lymphoma 6 inhibitor with IC50 of 212 μM.
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