A-443654
作者：齊岳
發(fā)布時(shí)間：2023-08-25
09:00:23
點(diǎn)擊數(shù)：
產(chǎn)品名稱：A-443654
產(chǎn)品描述：
| 產(chǎn)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). |
| 靶點(diǎn)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) |
| 體外活性 | 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]. |
| 體內(nèi)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 |
存儲
| 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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