ABT-199 (GDC-0199) is a new selective small molecule inhibitor of BCL-2 that appears to spare platelets while achieving potent antitumor activity. Proteins in the B cell CLL/lymphoma 2 (BCL-2) family are key regulators of the apoptotic process. As a single agent, ABT-199 was as effective as ABT-737 in prolonging survival of immunocompetent tumor-bearing mice without causing thrombocytopenia. ABT-199 (GDC-0199) is an engineered version of ABT-263 (Navitoclax) but with much better selectivity.
Biochem Pharmacol. 2023 Dec 10;220:115981.
Enhancing anti-AML activity of venetoclax by isoflavone ME-344 through suppression of OXPHOS and/or purine biosynthesis in vitro
ABT-199 (Venetoclax) purchased from AbMole
J Cell Mol Med. 2022 May;26(9):2646-2657.
Venetoclax enhances DNA damage induced by XPO1 inhibitors: A novel mechanism underlying the synergistic antileukaemic effect in acute myeloid leukaemia
ABT-199 (Venetoclax) purchased from AbMole
2020 Dec.
Zelluläre Seneszenz induziert durch neue zielgerichtete Therapien
ABT-199 (Venetoclax) purchased from AbMole
Cell Death and Disease. 2018 Jan 26;9:137-52.
Downregulation of MCL-1 and upregulation of PUMA using mTOR inhibitors enhance antitumor efficacy of BH3 mimetics in triple-negative breast cancer
ABT-199 (Venetoclax) purchased from AbMole
Oncotarget. 2016 Jan 26;7(4):4195-209.
Epigenetic modification of TLR4 promotes activation of NFκB by regulating methylCpGbinding domain protein 2 and Sp1 in gastric cancer.
ABT-199 (Venetoclax) purchased from AbMole
Cell Experiment | |
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Cell lines | CLL cells and platelets |
Preparation method | Apoptosis analysis Peripheral blood mononuclear cells were purified using Histopaque and cultured in RPMI 1640 medium supplemented with 10% fetal calf serum and 2 mmol/l L-glutamine at2*106 cells/ml. Cells were exposed to different concentrations of ABT-737, ABT-263, or ABT-199 for 4 h before analysis of apoptosis by externalisation of phosphatidylserine (PS) and binding of AnnexinV/fluorescein isothiocyanate (FITC). Platelets isolated from healthy volunteers were cultured in Hepes-buffered saline and exposed to different concentrations of ABT-737, ABT-263, or ABT-199 for 4 h before analysis of apoptosis in the CD41-positive population by externalisation of PS and binding of AnnexinV/FITC. |
Concentrations | 0~3µM |
Incubation time | 4 h |
Animal Experiment | |
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Animal models | C57BL/6 mice were injected (i.v.) with 3x106 T1 lymphoma cells |
Formulation | formulated in 60% phosal 50PG (standardized phosphatidylcholine concentrate with at least 50% PC and propylene glycol |
Dosages | 100 mg/kg |
Administration | oral gavage |
Molecular Weight | 868.44 |
Formula | C45H50ClN7O7S |
CAS Number | 1257044-40-8 |
Solubility (25°C) | DMSO 80 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
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