计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥95% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
RMC-5552 is a potent and selective mTORC1 inhibitor. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC 50 s of 0.14 nM and 0.48 nM, respectively. RMC-5552 shows much lower pAKT inhibition (IC 50 of 19 nM), resulting in mTORC1/mTORC2 selectivity approaching 40-fold. RMC-5552 has anti-cancer activity
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 T max (h) C max (ng/mL) C max (μM) AUC last (μg/mL × h) AUC last (μM × h) t 1/2 (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 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Balb/c nude mice (6-8 weeks of age) injected with MCF-7 cells Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg Administration: i.p.; once weekly; for 28 days Result: Resulted in a reduction in tumor volume.
Form:Solid
IC50& Target:mTORC1
规格
规格或纯度
≥95%
英文名称
RMC-5552
生化机理
RMC-5552 是一种强效的选择性 mTORC1 抑制剂。RMC-5552 可抑制 mTORC1 pS6K 和 p4EBP1 的磷酸化，其 IC 50 s 分别为 0.14 nM 和 0.48 nM。RMC-5552 对 pAKT 的抑制作用要低得多（IC 50 为 19 nM），从而导致 mTORC1/mTORC2 sele
储存条件
-20°C储存
运输条件
超低温运输
纯度
≥95%
名称和识别符
分子类型
小分子
Isomeric SMILES
C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H]([C@@H](C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)OC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCC(=O)N5CCC6=C(C5)C=CC(=C6)CN7C8=NC=NC(=C8C(=N7)C9=CC1=C(C=C9)OC(=N1)N)N)O)C)/C)O)OC)C)C)/C)OC
PubChem CID
分子量
1778.13
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 166.67 mg/mL (93.73 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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