ABT 263
Navitoclax
CAS: 923564-51-6
Molecular Formula: C47H55ClF3N5O6S3
ABT 263 - Names and Identifiers
| Name | Navitoclax |
| Synonyms | ABT263 CS-1871 ABT 263 ABT-263 CS-1967 NAVITOCLAX Navitoclax (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 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 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 (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 |
| CAS | 923564-51-6 |
ABT 263 - Physico-chemical Properties
| Molecular Formula | C47H55ClF3N5O6S3 |
| Molar Mass | 974.61 |
| Density | 1.41±0.1 g/cm3(Predicted) |
| Melting Point | 114-116°C |
| Solubility | Soluble in DMSO (up to 25 mg/ml). |
| Appearance | solid |
| Color | White |
| pKa | 4.60±0.10(Predicted) |
| Storage Condition | -20°C Freezer, Under Inert Atmosphere |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Use | ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2, and Bcl-w with Ki ≤ 0.5 nM,≤ 1 nM, and ≤ 1 nM, respectively, but weakly binds to Mcl-1 and A1. Phase 2. |
| In vitro study | ABT-263 potent inhibition of the Bcl-2 protein family, K I was 0.5, 1, and 1 nM when ABT-263 acted on Bcl-xL, Bcl-2, and Bcl-w, respectively, using fluorescence polarization analysis. ABT-263 is structurally related to ABT-737. ABT-263 blocks Bcl-2 and Bcl-XL interaction with the apoptosis precursor protein. Overexpression of Bcl-2, Bcl-2, and Bcl-XL of Mcl-1 family members is often associated with tumor repair and drug resistance. ABT-263 at Bcl-2 and Bcl-XL of The overexpression showed a protective effect with EC50 of 60 and 20 nM, respectively. ABT-263 different cells showed different cell activities, with an EC50 of 110nM in the H146 cell line and 22 μm in the H82 cell line. ABT-737 can effectively act on four cell lines with EC50 values <400 nM, namely H146, H889, H1963, and h1417. Two ABT-737 resistant cell lines, H1048 and H82, also showed ABT-263 resistance. |
| In vivo study | H345 transplanted tumor model was treated with ABT-263, according to animal body weight, 10mg per kilogram per day ABT-263, the results of tumor growth inhibition rate of 80%, tumor volume decreased by more than 50%, it showed a strong anti-cancer effect of ABT-263. ABT-263 in non small cell lung cancer and acute lymphoblastic leukemia model of transplanted tumor, the daily oral administration alone, the results show that the tumor complete regression. ABT-263 single effect on B- cell lymphoma and multiple myeloma model of transplanted tumor effect is not obvious, but can significantly enhance the clinical properties of other related drugs. |
ABT 263 - Risk and Safety
| HS Code | 29339900 |
ABT 263 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.026 ml | 5.13 ml | 10.261 ml |
| 5 mM | 0.205 ml | 1.026 ml | 2.052 ml |
| 10 mM | 0.103 ml | 0.513 ml | 1.026 ml |
| 5 mM | 0.021 ml | 0.103 ml | 0.205 ml |
Last Update：2024-01-02 23:10:35
ABT 263 - Reference Information
| use | ABT 263 is a new inhibitor of anti-apoptotic BCL-2 protein. A promising new anti-cancer drug. It is a potent Bcl-2 family inhibitor. |
| biological activity | Navitoclax (ABT-263) is an effective inhibitor of Bcl-xL,Bcl-2 and Bcl-w. Ki is ≤ 0.5 nM,≤ 1 nM and ≤ 1 nM respectively in cell-free test, but it is weakly bound to Mcl-1 and A1. Phase 2. |
| target | TargetValue Bcl-xL <= 0.5 nM(Ki) Bcl-2 <= 1 nM(Ki) Bcl-w <= 1 nM(Ki) <= 1 nM(Ki) |
| Target | Value |
| Bcl-xL (Cell-free assay) | <=0.5 nM(Ki) |
| Bcl-2 (Cell-free assay) | <=1 nM(Ki) |
| Bcl-w (Cell-free assay) | <= 1 nM(Ki) |
| in vitro study | ABT-263 effectively inhibit Bcl-2 protein family. when fluorescence polarization analysis was used to test ABT-263 acting on Bcl-xL, Bcl-2 and Bcl-w, K I was 0.5, 1 and 1 nM respectively. ABT-263 is structurally related to ABT-737. ABT-263 blocking Bcl-2 and Bcl-XL interactions with apoptotic precursor proteins. Overexpression of Bcl-2,Bcl-XL, and Mcl-1 of Bcl-2 family members is usually related to tumor repair and drug resistance. ABT-263 showed protective effects when acting on overexpressed Bcl-2 and Bcl-XL, with EC50 of 60 and 20 nM respectively. ABT-263 showed different cell activity when acting on different cells, the EC50 was 110nM when acting on the H146 cell line, and the EC50 was 22 µM when acting on the H82 cell line. ABT-737 can effectively act on four cell lines with EC50 values <400 nM, namely H146, H889, H1963, and H1417. Two anti-ABT-737 cell lines, namely H1048 and H82, also showed anti-ABT-263 properties. |
| in vivo study | H345 transplanted tumor model was treated with ABT-263, and 10mg of ABT-263 per kilogram per day was treated according to animal body weight. as a result, the tumor growth inhibition rate reached 80% and the tumor volume was reduced by more than 50%, showing a ABT-263 strong anti-cancer effect. When ABT-263 acted on transplanted tumor models of non-small cell lung cancer and acute lymphoblastic leukemia, it was taken orally alone every day, and the results showed complete tumor decline. ABT-263 the effect of acting alone on the transplanted tumor model of B- cell lymphoma and multiple myeloma is not obvious, it can significantly enhance the drug properties of other clinical related drugs. |
Last Update：2024-04-09 21:54:55
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Spot supply
Product Name: Navitoclax Visit Supplier Webpage Request for quotationCAS: 923564-51-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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