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- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
2382768-62-7
- 规格:
1 mg
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RMC-5552
CAS No. : 2382768-62-7
MCE 国际站:RMC-5552
产品活性:RMC-5552 是一种有效的选择性 mTORC1 抑制剂。RMC-5552 抑制 mTORC1 pS6K 和 p4EBP1 的磷酸化,IC50 分别为 0.14 nM 和 0.48 nM。RMC-5552 表现出低得多的 pAKT 抑制作用 (IC50 为 19 nM),导致 mTORC1/mTORC2 选择性接近 40 倍。RMC-5552 具有抗癌活性。
研究领域:PI3K/Akt/mTOR
作用靶点:mTOR
In Vitro: The presence of FKBP12, whose recruitment would only be observed in the presence of the FKBP12-FRB allosteric modality of RMC-5552. Density for RMC-5552 is evident at the interface between FKBP12 and the FRB domain of mTOR. RMC-5552 makes hydrogen bonds to the backbone of G2238 and V2240, the “hinge” of mTOR, via the 4-aminopyrazolo[3,4-d]pyrimidine core, and the 2-aminobenzoxazole makes hydrogen-bonding interactions to E2190 and K2187.
In Vivo: RMC-5552 (1-10 mg/kg; i.p.; once weekly; for 28 days) exhibits antitumor activity in a human xenograft model of MCF-7 breast cancer in mice in vivo.
PK Parameters of RMC-5552 38 in Mice at 1 mg/kg via IP Administration
| compounds | Tmax (h) | Cmax (ng/mL) | Cmax (μM) | AUClast (μg/mL × h) | AUClast (μM × h) | t1/2 (h) |
| 38 RMC-5552 | 2.0 ± 0.0 | 5667 ± 1106 | 3.19 ± 0.62 | 46 089 ± 5320 | 25.9 ± 3.0 | 4.8 ± 0.4 |
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文献和实验maltose mcrA = Mutation eliminating restriction of DNA methylated at the sequence CmCGG (possibly mCG). Carried on the e14 prophage (q.v.) mcrB = Mutation eliminating restriction of DNA methylated at the sequence RmC metB = requires methionine metC
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Multicolour 3D-FISH in vertebrate cells
money and insures higher flexibility in designing experiments. An official source to obtain chromosome specific DNA probes is provided by M. Rocchi, University of Bari (http://www.biologia.uniba.it/rmc/). In the following section we present
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