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Formula | C42H45ClN6O5S2 |
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Molecular Weight | 813.43 | CAS No. | 852808-04-9 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (122.93 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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 | ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2. | ||||||||
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In vitro | ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. ABT-737 is sensitive to HL60, KG1 and NB4 cells with IC50 of 50 nM, 80 nM and 80 nM, respectively. ABT-737 induces apoptosis in HL60 cells, which due to decreased Bcl-2/Bax heterodimerization and has no effect on cell cycle distribution. ABT-737 also induces cytochrome c release from purified mitochondria and promotes conformational changes in Bax that are associated with apoptosis. [1] Resistant cells (Hela and MCF-7) can be sensitized to ABT-737 by approaches that down-regulate, destabilize, or inactivate Mcl-1. ABT-737 also causes Bax/BAK-dependent cytochrome c release only when Mcl-1 has been neutralized. [2] ABT-737 displaces Bim from Bcl2's BH3-binding pocket, allowing Bim to activate Bax, induce mitochondrial permeabilization, and rapidly commit the primary chronic lymphocytic leukemia (CLL) cells to death. [3] Knockdown of Mcl-1 with siRNA sensitizes two resistant SCLC cell lines H196 and DMS114 to ABT-737 by enhancing the induction of apoptosis. Likewise, up-regulation of Noxa sensitizes H196 cells to ABT-737. ABT-737 inhibits proliferation and induces apoptosis in many SCLC cell lines including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 and etc. Bcl-2 and Noxa may contribute mechanistically to the cellular response to ABT-737 in NCI-H146 cells. [4] A recent study shows that ABT-737 significantly induces apoptosis in HTLV-1 infected T-cell lines as well as in fresh ATLL cells. [5] | ||||||||
In vivo | In aggressive leukemia model, ABT-737 suppresses the leukemia burden by 53% at the 30 mg/kg, with significantly extended survival of mice. ABT-737 does not induce significantly abnormalities in blood cell counts or serum chemistries. [1] ABT-737 prolongs the survival of recipient mice transplanted with Bcl-2-transduced tumors. [2] ABT-737 shows great antitumor activity in an ATLL mouse model at a dose of 100 mg/kg. [5] | ||||||||
Features | First-generation inhibitor of anti-apoptotic Bcl-2 proteins. |
Kinase Assay: |
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Data from [Nat Med, 2013, 19(11), 1478-88]
Data from [Cell Death Dis, 2013, 4, e801]
Data from [Biochem Biophys Res Commun, 2013, 408, 344-9]
Data from [Biochem Biophys Res Commun, 2012, 408, 344-9]
Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] | PubMed: 38262581 |
Mitophagy curtails cytosolic mtDNA-dependent activation of cGAS/STING inflammation during aging [ Nat Commun, 2024, 15(1):830] | PubMed: 38280852 |
Detection of senescence using machine learning algorithms based on nuclear features [ Nat Commun, 2024, 15(1):1041] | PubMed: 38310113 |
BH3 mimetics and azacitidine show synergistic effects on juvenile myelomonocytic leukemia [ Leukemia, 2024, 38(1):136-148] | PubMed: 37945692 |
Inhibitor PF-04691502 works as a senolytic to regulate cellular senescence [ Exp Gerontol, 2024, 186:112359] | PubMed: 38184267 |
Tau activation of microglial cGAS-IFN reduces MEF2C-mediated cognitive resilience [ Nat Neurosci, 2023, 26(5):737-750] | PubMed: 37095396 |
Intracellular FGF1 protects cells from apoptosis through direct interaction with p53 [ Cell Mol Life Sci, 2023, 80(10):311] | PubMed: 37783936 |
STING agonism turns human T cells into interferon-producing cells but impedes their functionality [ EMBO Rep, 2023, e55536.] | PubMed: 36705069 |
HPV-induced host epigenetic reprogramming is lost upon progression to high-grade cervical intraepithelial neoplasia [ Int J Cancer, 2023, 152(11):2321-2330] | PubMed: 36810770 |
SARS-CoV-2 E and 3a Proteins Are Inducers of Pannexin Currents [ Cells, 2023, 12(11)1474] | PubMed: 37296595 |
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