Navitoclax [923564-51-6]

Katalog-Nummer HY-10087-500mg

Size : 500mg

Marke : MedChemExpress

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Navitoclax (ABT-263) est un protéine de la famille Bcl-2 puissant et actif par voie orale qui se lie à de multiples protéines anti-apoptotiques de la famille Bcl-2, telles que Bcl-xL, Bcl-2 et Bcl-w, avec un Ki inférieur à 1 nM.

Navitoclax (ABT-263) ist ein wirksamer und oral wirksamer Proteininhibitor der Bcl-2-Familie, der an mehrere antiapoptotische Proteine ​​der Bcl-2-Familie wie Bcl-xL, Bcl-2 und Bcl-w mit einem Ki von weniger bindet als 1 nM.

Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM.

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Navitoclax Chemische Struktur

CAS. Nr. : 923564-51-6

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Proliferation Assay
WB
    Cells are treated with 25 nM siRNA for 48 hours followed by 1 μM ABT-263 for 36 hours.
    Combination treatment. (a) Comparison of AZD-8055 and ABT-263 treatment in all cell lines. Red indicates sensitivity, while blue indicates resistance. (b) Depiction of synergism where the values shown are excess over Bliss Independence, a prediction of inhibition without synergism. Increased synergism is evident by an increased number, shown in red, while negative numbers in blue represent an antagonistic effect.
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    Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM.

    Bcl-W

    1 nM (Ki)

    Bcl-xL

    1 nM (Ki)

    Bcl-2

    1 nM (Ki)

    In Vitro

    Navitoclax (ABT-263) is active against approximately one-half of the cell lines of the PPTP in vitro panel. The median IC50 for all of the lines in the panel is 1.91 μM. Navitoclax in combination with chemotherapy agents leads most ovarian cancer cell lines a synergistic response, and enhances the caspase activation in both SK-OV-3 and IGROV-1 cell lines.

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    • [1]. Lock R1, et al. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jun;50(6):1181-1189.  [Content Brief]

      [2]. Wong M, et al. Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models.Mol Cancer Ther. 2012 Apr;11(4):1026-1035.  [Content Brief]

      [3]. Chen J, et al. The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Mol Cancer Ther. 2011 Dec;10(12):2340-9.  [Content Brief]

    • [1]. Lock R1, et al. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jun;50(6):1181-1189.

      [2]. Wong M, et al. Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models.Mol Cancer Ther. 2012 Apr;11(4):1026-1035.

      [3]. Chen J, et al. The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Mol Cancer Ther. 2011 Dec;10(12):2340-9.

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / DMF 1 mM 1.0261 mL 5.1303 mL 10.2605 mL 25.6513 mL
    5 mM 0.2052 mL 1.0261 mL 2.0521 mL 5.1303 mL
    10 mM 0.1026 mL 0.5130 mL 1.0261 mL 2.5651 mL
    15 mM 0.0684 mL 0.3420 mL 0.6840 mL 1.7101 mL
    20 mM 0.0513 mL 0.2565 mL 0.5130 mL 1.2826 mL
    25 mM 0.0410 mL 0.2052 mL 0.4104 mL 1.0261 mL
    30 mM 0.0342 mL 0.1710 mL 0.3420 mL 0.8550 mL
    40 mM 0.0257 mL 0.1283 mL 0.2565 mL 0.6413 mL
    50 mM 0.0205 mL 0.1026 mL 0.2052 mL 0.5130 mL
    60 mM 0.0171 mL 0.0855 mL 0.1710 mL 0.4275 mL
    DMF 80 mM 0.0128 mL 0.0641 mL 0.1283 mL 0.3206 mL
    100 mM 0.0103 mL 0.0513 mL 0.1026 mL 0.2565 mL
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    • Apoptosis
    • Bcl-2 Family
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Navitoclax923564-51-6ABT-263ABT263ABT 263Bcl-2 FamilyInhibitorinhibitorinhibit

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    Produktname:
    Navitoclax
    Art. -Nr.:
    HY-10087
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