|Source||Mol Cancer Res (2015). Figure 4. Chelerythrine|
|Method||Cell proliferation assay|
|Cell Lines||621-101 cells|
|Incubation Time||2 h|
|Results||CI-1040 pretreatment did not abrogate the effects of chelerythrine chloride in 621-101 cells or Tsc2-null MEFs|
|Source||Mol Cancer Res (2015). Figure 3. Chelerythrine|
|Cell Lines||Tsc2+/+ MEFs|
|Incubation Time||4 h|
|Results||Chelerythrine chloride induced PARP cleavage in Tsc2-null MEFs but not Tsc2-expressing MEFs.|
|Preparation method||For the phosphorylation by [32P]Pi, 100 lgmL1 SRV protein in an E2-favoring reaction buffer (20 mM MES-pH 6.0-with 10 mM MgCl2, 2 mM EGTA, and the indicated chelerythrine concentrations) was incubated and 4 mM [32P]Pi were added.|
|Concentrations||1, 10, 50 and 100 μM|
|Incubation time||20–40 min,|
|Animal models||BALB/c (H2d) mice|
|Dosages||25, 50, 100, and 200 mg/kg|
|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 2 mg/mL|
Chelerythrine delayed tumor growth and increased survival duration of Dalton's lymphoma bearing BALB/c H(2d) mice by activation of NK cells in vivo.
Kumar S, et al. J Cancer Res Ther. 2015 Oct-Dec;11(4):904-10. PMID: 26881539.
Chelerythrine inhibits the sarco/endoplasmic reticulum Ca(2+)-ATPase and results in cell Ca(2+) imbalance.
Vieira SM, et al. Arch Biochem Biophys. 2015 Mar 15;570:58-65. PMID: 25721495.
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