852808-04-9
ABT-737
CAS: 852808-04-9
Molecular Formula: C42H45ClN6O5S2
852808-04-9 - Names and Identifiers
| Name | ABT-737 |
| Synonyms | ABT-737 ABT 737 4-{4-[(4'-Chlorobiphenyl-2-yl)Methyl]piperazin-1-yl}-N-[(4-{[(2R)-4-(diMethylaMino)-1- (R)-4-(4-((4'-chlorobiphenyl-2-yl)Methyl)piperazin-1-yl)-N-(4-(4-(diMethylaMino)-1-(phenylthio)butan-2-ylaMino)-3-nitrophenylsulfonyl)benzaMide 4-{4-[(4'-Chlorobiphenyl-2-yl)Methyl]piperazin-1-yl}-N-[(4-{[(2R)-4-(diMethylaMino)-1-(phenylsulfanyl)butan-2-yl]aMino}-3-nitrophenyl)sulfonyl]benzaMide 4-[4-[(4'-Chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]benzamide BenzaMide, 4-[4-[(4'-chloro[1,1'-biphenyl]-2-yl)Methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(diMethylaMino)-1-[(phenylthio)Methyl]propyl]aMino]-3-nitrophenyl]sulfonyl]- 4-[4-[(4'-Chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]benzamide ABT-737 |
| CAS | 852808-04-9 |
852808-04-9 - Physico-chemical Properties
| Molecular Formula | C42H45ClN6O5S2 |
| Molar Mass | 813.43 |
| Melting Point | 152-154°C |
| Solubility | DMSO (Slightly), Methanol (Slightly, Heated, Sonicated) |
| Appearance | Yellow solid |
| Color | Light Yellow to Yellow |
| Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| In vitro study | ABT-737 reduced the BCL-2/BAX heterodimer while inducing apoptosis in HL60 cells, but had no inhibitory effect on cell cycle distribution. ABT-737 also induces the release of cytochrome C from mitochondria and promotes the conformational change of BAX, which is associated with apoptosis. In a leukemia model, ABT-737 treatment at 30 mg/kg blocked 53% of the leukemia burden and significantly prolonged the lifespan of the mice. ABT-737 will not lead to abnormal blood cell count and serum composition. The resistant cells (Hela and Mcl-1) were sensitized to MCF-7 by inactivating ABT-737. When Mcl-1 was ineffective, ABT-737 also resulted in BAX/BAK-dependent cytochrome C release. ABT-737 to extend the life of mice carrying BCL-2 tumor. ABT-737 BIM was replaced from the BCL2's BH3 binding pocket, so that BIM activated BAX, induced mitochondrial permeabilization, rapid death of chronic lymphocytic leukemia (CLL) cells. Noxa positive regulation enhanced the sensitivity of H196 cells to ABT-737. ABT-737 inhibits the proliferation of various SCLC cell lines, including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, etc., and induces apoptosis. Recent studies have shown that ABT-737 of ATLL cells significantly induce apoptosis in HTLV-1 of infected T cells. ABT-737 at a dose of 100 mg/kg in the ATLL mouse model showed strong anticancer activity. |
| In vivo study | In ABT-737, the leukemia burden was inhibited by 53% at the dose of 30 mg/kg in the leukemia model, and the life span of the mice was significantly prolonged. ABT-737 does not cause changes in blood cell count and plasma chemistry. ABT-737 prolong the life span of mice transplanted with BCL-2 sensor tumors. ABT-737 at a dose of 100 mg/kg, the ATLL mouse model has strong anticancer activity. |
852808-04-9 - Risk and Safety
| HS Code | 29309090 |
852808-04-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.229 ml | 6.147 ml | 12.294 ml |
| 5 mM | 0.246 ml | 1.229 ml | 2.459 ml |
| 10 mM | 0.123 ml | 0.615 ml | 1.229 ml |
| 5 mM | 0.025 ml | 0.123 ml | 0.246 ml |
Last Update：2024-01-02 23:10:35
852808-04-9 - Reference Information
| introduction | ABT-737 is a BH3 analog inhibitor that acts on Bcl-xL,Bcl-2 and Bcl-w. EC50 is 78.7nM,30.3nM and 197.8nM respectively in cell-free test. However, it has no inhibitory effect on Mcl-1,Bcl-B and Bfl-1. |
| biological activity | ABT-737 is a BH3 mimetic inhibitor that acts on Bcl-xL,Bcl-2 and Bcl-w. EC50 is 78.7 nM,30.3 nM and 197.8 nM respectively in cell-free test. However, it has no inhibitory effect on Mcl-1, Bcl-B and Bfl-1. ABT737 up-regulates the expression of apoptosis-related gene Bim through JNK/c-Jun signaling pathway, inducing apoptosis in Hela cells. MTT assay was used to detect the growth inhibitory effect of ABT-737 on human cervical cancer Hela cells. Flow cytometry was used to detect the apoptosis rate. The expression of JNK, phospho-JNK, c-Jun, phospho-c-Jun and Bim protein were detected by Western blot. The changes of Bim at mRNA level were detected by RT-PCR. Transient transfection of JNK specific inhibitor SP600125 and siRNA inhibited the activities of JNK and c-Jun. ABT-737 can inhibit the growth of Hela cells and induce apoptosis of HeLa cells. ABT737 can activate JNK kinase activity and its downstream target molecule c-Jun, and the expression of apoptosis-related gene Bim at mRNA level and protein level is also up-regulated. After JNK-specific inhibitors were used to SP600125 and target JNK and c-Jun siRNA to inhibit the activity or expression of JNK or c-Jun, ABT737-induced up-regulation of Bim and apoptosis were also effectively blocked. ABT-737 is a BH3 mimetic inhibitor, which acts on Bcl-xL,Bcl-2 and Bcl-w. EC50 is 78.7 nM,30.3 nM and 197.8 nM respectively in cell-free test. However, it has no inhibitory effect on Mcl-1, Bcl-B and Bfl-1. ABT-737 can induce apoptosis and mitochondrial autophagy in mitochondrial pathway. Phase 2. |
| features | ABT-737 are small molecule inhibitors of the first generation of anti-apoptotic BCL-2 family proteins. |
| target | TargetValue Bcl-2 (Cell-free assay) 30.3 nM(EC50) Bcl-xL (Cell-free assay) 78.7 nM(EC50) Bcl-w (Cell-free assay) 197.8 nM(EC50) Bcl-B (Cell-free assay) 1.82 μM(EC50) |
| Target | Value |
| Bcl-2 (Cell-free assay) | 30.3 nM(EC50) |
| Bcl-xL (Cell-free assay) | 78.7 nM(EC50) |
| Bcl-w (Cell-free assay) | 197.8 nM(EC50) |
| Bcl-B (Cell-free assay) | 1.82 μM(EC50) |
| in vitro study | ABT-737 reduce BCL-2/BAX heterodimer and induce HL60 cell apoptosis, but it has no inhibitory effect on cell cycle distribution. ABT-737 also induces the release of cytochrome C from mitochondria and promotes conformational changes in BAX, which is associated with apoptosis. In the leukemia model, the ABT-737 was treated at 30 mg/kg to block the 53% leukemia load and significantly prolong the lifespan of the mice. ABT-737 does not cause abnormalities in blood cell count and serum composition. Resistance cells (Hela and MCF-7) are sensitized to ABT-737 by inactivating Mcl-1. When the Mcl-1 is ineffective, ABT-737 also leads to BAX/BAK-dependent cytochrome C release. ABT-737 prolong the life of mice carrying BCL-2 tumors. ABT-737 replacing BIM from BCL2's BH3 binding bag, BIM activates BAX, induces mitochondrial permeabilization, and rapidly kills chronic lymphocytic leukemia (CLL) cells. Noxa positive regulation enhances the sensitivity of H196 cells to ABT-737. ABT-737 inhibit the proliferation of various SCLC cell lines, including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, etc., and induce apoptosis. Recent studies have shown that ABT-737 acts on ATLL cells and obviously induces apoptosis of HTLV-1 infected T cells. ABT-737 showed strong anticancer activity on ATLL mouse model at a dose of 100 mg/kg. |
| in vivo study | ABT-737 acted on the leukemia model at a dose of 30 mg/kg, inhibiting the burden of leukemia by 53%, and obviously prolonging the life of mice. ABT-737 will not cause changes in blood cell count and plasma chemistry. ABT-737 prolong the life of mice with transplanted BCL-2 sensing tumors. ABT-737 has strong anticancer activity on ATLL mouse model at a dose of 100 mg/kg. |
Last Update：2024-04-09 21:21:28
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Product Name: ABT-737 Visit Supplier Webpage Request for quotationCAS: 852808-04-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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