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Formula | C45H50ClN7O7S |
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Molecular Weight | 868.44 | CAS No. | 1257044-40-8 | ||||||||
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (115.14 mM) | ||||||||
Water | Insoluble | ||||||||||
Ethanol | Insoluble | ||||||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3. | ||
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Targets |
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In vitro | ABT-199 shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with Ki of 48 nM, > 444 nM and 245 nM, respectively. ABT-199 potently inhibits FL5.12-Bcl-2 cells, RS4;11 cells with EC50 of 4 nM and 8 nM, while shows low activity against FL5.12-Bcl-xL cells with EC50 of 261 nM. ABT-199 induces a rapid apoptosis in RS4;11 cells with cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA. Quantitative immunoblotting reveals that sensitivity to ABT-199 correlated strongly with the expression of Bcl-2, including NHL, DLBCL, MCL, AML and ALL cell lines. ABT-199 also induces apoptosis in CLL with an average EC50 of 3.0 nM. [1] | ||
In vivo | ABT-199 (100 mg/kg) causes a maximal tumor growth inhibition of 95% and tumor growth delay of 152% in RS4;11 xenografts. ABT-199 also inhibits xenograft growth (DoHH2, Granta-519) as a single agent or in combination with SDX-105 and other agents. [1] | ||
Features | Re-engineered version of ABT-263 (Navitoclax). |
Kinase Assay:[1] |
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Cell Assay:[1] |
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Animal Study:[1] |
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Data from [Data independently produced by Mol Oncol, 2014, 10.1016/j.molonc.2014.09.008]
Data from [J Biol Chem, 2014, 289(23), 16190-9]
Data from [Data independently produced by , , Blood, 2015, 126(11):1346-56]
Data from [Data independently produced by , , Leukemia, 2017, 31(11):2336-2346]
RAS-mutant leukaemia stem cells drive clinical resistance to venetoclax [ Nature, 2024, ] | PubMed: 39478230 |
Dual blockade of IL-10 and PD-1 leads to control of SIV viral rebound following analytical treatment interruption [ Nat Immunol, 2024, 10.1038/s41590-024-01952-4] | PubMed: 39266691 |
Proteasome inhibition enhances the anti-leukemic efficacy of chimeric antigen receptor (CAR) expressing NK cells against acute myeloid leukemia [ J Hematol Oncol, 2024, 17(1):85] | PubMed: 39285441 |
Comprehensive characterization of IFNγ signaling in acute myeloid leukemia reveals prognostic and therapeutic strategies [ Nat Commun, 2024, 15(1):1821] | PubMed: 38418901 |
AXL-specific single domain antibodies show diagnostic potential and anti-tumor activity in Acute Myeloid Leukemia [ Theranostics, 2024, 14(7):2656-2674] | PubMed: 38773967 |
AXL-specific single domain antibodies show diagnostic potential and anti-tumor activity in Acute Myeloid Leukemia [ Theranostics, 2024, 14(7):2656-2674] | PubMed: 38773967 |
BH3 mimetics and azacitidine show synergistic effects on juvenile myelomonocytic leukemia [ Leukemia, 2024, 38(1):136-148] | PubMed: 37945692 |
8-Cl-Ado and 8-NH2-Ado synergize with venetoclax to target the methionine-MAT2A-SAM axis in acute myeloid leukemia [ Leukemia, 2024, 10.1038/s41375-024-02222-w] | PubMed: 38643304 |
Targeting BCL2 with Venetoclax Enhances the Efficacy of the KRASG12D Inhibitor MRTX1133 in Pancreatic Cancer [ Cancer Res, 2024, 10.1158/0008-5472.CAN-23-3574] | PubMed: 39137400 |
Dual ON/OFF-switch chimeric antigen receptor controlled by two clinically approved drugs [ Proc Natl Acad Sci U S A, 2024, 121(44):e2405085121] | PubMed: 39453747 |
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Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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