| Company Name: |
Guangzhou Isun Pharmaceutical Co., Ltd Gold |
| Tel: |
020-39119399 18927568969 |
| Email: |
isunpharm@qq.com |
| Products Intro: |
Product Name:Navitoclax(ABT-263)
CAS:923564-51-6
Purity:98% Package:1G; 5G; 25G; 100G; 1KG; 5KG
|
| Company Name: |
Zhengzhou HSH Science & Technology Co., Ltd. Gold |
| Tel: |
0371-55932928 18937192232; |
| Email: |
1282296214@qq.com |
| Products Intro: |
Product Name:4-[4-[[2-(4-Chlorophenyl)-5,5-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(4-morpholinyl)-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]phenyl]sulfonyl]benzamide;ABT 263;Navitoclax
CAS:923564-51-6
Purity:98% HPLC Package:100g;10g;5g;1g;500mg;250mg;100mg;10mg;5mg
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- Navitoclax
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- $39.00
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2026-08-20
- CAS:923564-51-6
- Purity: 98.88%
- Supply Ability: 10g
- ABT 263
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- $2.00
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2019-07-06
- CAS:923564-51-6
- Min. Order: 1KG
- Purity: 99%
Related articles - ABT-263
- Navitoclax, also known as ABT-263 and ABT 263, is a potent, oral biologically active inhibitor of the Bcl-2 protein family, ac....
- Oct 28，2021
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| Product Name: | ABT-263 | | Synonyms: | ABT263;ABT-263;4-[4-[[2-(4-chlorophenyl)-5,5-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-n-[4-[[(2r)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide;(R)-4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-(4-morpholino-1-(phenylthio)butan-2-ylamino)-3-(trifluoromethylsulfonyl)phenylsulfonyl)benzamide;NAVITOCLAX;ABT 263;ABT263;(R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide;4-[4-[[2-(4-Chlorophenyl)-5,5-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(4-morpholinyl)-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]phenyl]sulfonyl]benzamide;BenzaMide, 4-(4-((2-(4-chlorophenyl)-5,5-diMe;Navitoclax (ABT-263) | | CAS: | 923564-51-6 | | MF: | C47H55ClF3N5O6S3 | | MW: | 974.62 | | EINECS: | | | Product Categories: | Inhibitor;Apis;Chiral Reagents;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds | | Mol File: | 923564-51-6.mol |  |
| | ABT-263 Chemical Properties |
| Melting point | 114-116°C | | density | 1.41±0.1 g/cm3(Predicted) | | storage temp. | -20°C Freezer, Under Inert Atmosphere | | solubility | Soluble in DMSO (up to 25 mg/ml). | | form | solid | | pka | 4.60±0.10(Predicted) | | color | White | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. | | InChIKey | JLYAXFNOILIKPP-KXQOOQHDSA-N | | SMILES | C(NS(C1=CC=C(N[C@@H](CSC2=CC=CC=C2)CCN2CCOCC2)C(S(C(F)(F)F)(=O)=O)=C1)(=O)=O)(=O)C1=CC=C(N2CCN(CC3CC(C)(C)CCC=3C3=CC=C(Cl)C=C3)CC2)C=C1 | | CAS DataBase Reference | 923564-51-6 |
| | ABT-263 Usage And Synthesis |
| Description | ABT-263 (923564-51-6) is a potent and selective Bcl-2 family inhibitor / BH3 domain mimetic which binds to Bcl-2, Bcl-xLand Bcl-w (Ki<1 nM). A useful tool compound which has shown interesting results in various cancer clinical trials.2Synergizes with deoxyglucose and other agents, inducing apoptosis in cancer cells in a xenograft mouse model.3A novel senolytic agent, inducing apoptosis preferentially in senescent cells in a cell type-restricted manner.4 | | Chemical Properties | Pale Yellow Solid | | Uses | ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤ 1 nM, respectively. | | Uses | A novel inhibitor of antiapoptotic BCL-2 proteins; a new promising anticancer drug candidate. | | Definition | ChEBI: Navitoclax is a N-sulfonylcarboxamide resulting from the formal condensation of the carboxy group of 4-{4-[(4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro[biphenyl]-2-yl)methyl]piperazin-1-yl}benzoic acid with the amino group of 4-{[(2R)-4-(morpholin-4-yl)-1-(phenylsulfanyl)butan-2-yl]amino}-3-[(trifluoromethyl)sulfonyl]benzenesulfonamide. It is a BH3-mimetic drug which targets the anti-apoptotic B-cell lymphoma-2 (BCL-2) family proteins, including BCL-2, BCL-xL, and BCL-w, and induces apoptosis in cancer cells. Currently under clinical investigation as treatment for solid tumors and hematologic malignancies. It has a role as a B-cell lymphoma 2 inhibitor, an apoptosis inducer and an antineoplastic agent. It is a member of piperazines, a member of monochlorobenzenes, a member of morpholines, an aryl sulfide, a N-sulfonylcarboxamide, a sulfone, an organofluorine compound, a secondary amino compound and a tertiary amino compound. | | Mechanism of action | ABT‐263 exerts its senolytic activity in senescent tumor cells by inhibiting BCL‐XL's interaction with BAX. ABT‐263 is a BH3 mimetic that inhibits anti‐apoptotic BCL‐2 family proteins by impeding their ability to bind pro‐apoptotic proteins, such as BAK and BAX. BCL‐2 and BCL‐XL are the primary targets of ABT‐263 in cancer cells. | | Pharmacokinetics | The pharmacokinetic profile of ABT-263 is characterized by low plasma clearance values and low volumes of distribution in mice, rats, dogs, and monkeys, with plasma elimination half-lives after i.v. Dose of 4.6 to 8.4 hours. Bioavailability after oral gavage was ～20% in all four species. Due to its low aqueous solubility, ABT-263 displays a prolonged dissolution rate-limited oral absorption. P.o. administration in lipid-based formulations, in which the compound is significantly more soluble, yields enhanced absorption with bioavailability near 50% and an oral elimination half-life of 8.9 hours in dogs[5].
| | in vitro | ABT-263 is structurally related to ABT-737; it is a disruptor of Bcl-2/Bcl-xL interactions with pro-apoptotic proteins. Overexpression of the prosurvival Bcl-2 family members is commonly associated with tumor maintenance, progression, and chemoresistance. [1] ABT-263 displays the protection afforded by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, respectively. A wide range of cellular activity is observed with ABT-263 having a 50% growth inhibition (EC50) of 110 nM against the most sensitive line (H146), whereas its activity in the least sensitive line (H82) results in an EC50 at 22 μM. All four cell lines with EC50 values of <400 nM (H146, H889, H1963, and H1417) are also highly sensitive to ABT-737, and the two most resistant lines (H1048 and H82) are similarly resistant to ABT-263. | | storage | Store at -20°C | | Background | ABT-263 is a potent and orally bioavailable Bcl-2 family inhibitor. This small molecule mimetic of BH3 domains specifically binds to Bcl-2, Bcl-xL, and Bcl-W with a Ki value of less than 1 nM. ABT-263 has been shown to have antitumor effects on small cell lung cancer xenograft models, resulting in complete tumor regression in some cases. Studies have shown that ABT-263 can enhance the effectiveness of chemotherapeutic and targeted agents against solid tumors. ABT-263 induces apoptosis, particularly in certain types of senescent cells. | | References | [1] Tse et al. (2008), ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor; Cancer Res., 68: 3421.
[2] Vogler et al. (2009), Bcl-2 inhibitors: small molecules with a big impact on cancer therapy; Cell Death Differ., 16: 360.
[3] Yamaguchi et al. (2011), Efficient elimination of cancer cells by deoxyglucose-ABT-263/737 combination therapy; PLoS ONE, 6(9): e24102.
[4] Zhu et al. (2016), Identification of a novel senolytic agent, navitoclax, targeting the Bcl-2 family of anti-apoptotic factors; Aging Cell, 15: 428.
[5] Tse et al. (2023), Data from ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor. |
| | ABT-263 Preparation Products And Raw materials |
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