A-443654
作者：齐岳
发布时间：2023-08-25
09:00:23
点击数：
产品名称：A-443654
产品描述：
| 产品描述 | A-443654 is a pan-Akt inhibitor. A-443654 has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM). |
| 靶点活性 | CK2:2.4 μM (ki), Chk1:2.3 μM (ki), cKIT:1.2 μM (ki), ERK2:340 nM (ki), Akt3:160 pM (ki), PKCδ:33 nM (ki), PKCγ:24 nM (ki), MAPK-AP2:3.3 μM (ki), KDR:3.1 μM (ki), PKA:6.3 nM (ki), CDK2:24 nM (ki), RSK2:11 nM (ki), Akt2:160 pM (ki), Src:2.6 μM (ki), Akt1:160 pM (ki), GSK3β:41 nM (ki) |
| 体外活性 | A-443654 exhibits a Ki of 160 pM which is a 30,000-fold improvement in potency versus the initial lead molecule. A-443654 reduces the P-GSK3 in a dose-responsive manner in all three cell lines. A-443654 is 40-fold selective for Akt over PKA, and it inhibits Akt1, Akt2, or Akt3 equally within cells. A-443654-induced morphological changes occur very rapidly (within 2 to 4 h) in both 10A and 10CA1a cells, with 10CA1a cells more sensitive to A-443654 than the 10A cells. A-443654 inhibits the proliferation of tumor cells with EC50 of 0.1 μM[1]. A-443654 demonstrates the greatest selective effect on the mutant cells compared to the WT cells with greater than 3.5 fold relative growth inhibition of the mutant cells[3]. FACScan Analysis of rapamycin and A-443654 effects on DNA content in 10A and 10CA1a cells. In contrast, A-443654 at 2 and 5 μM decreases Bcl-2 levels by 30 to 40% in the 10CA1a cells at 8h. The combination of rapamycin with 2 or 5 μM A-443654, however, markedly decreases Bcl-2 protein levels by appr 40 to 50% in the 10A cells and by appr 70% in the 10CA1a cells, respectively. A-443654 alone at 2 μM causes the 10CA1a cells, but not the 10A cells, to detach from the plate after 12 h, whereas 1 μM of A-443654 causes 10CA1a cells to detach from the plate after 12 h [2]. |
| 体内活性 | A-443654 (7.5 mg/kg/d, s.c.) inhibits tumor growth in the 3T3-Akt1 flank tumor model. A-443654 (30 mg/kg, s.c.) caused increased levels of phosphorylated Akt1 in MiaPaCa-2 tumors. A-443654 (50 mg/kg, s.c.) induces apoptosis in 3T3-Akt1 flank tumors [1]. |
| 分子量 | 397.47 |
| 分子式 | C24H23N5O |
| CAS No. | 552325-16-3 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 100 mg/mL (251.59 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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