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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Torkinib (PP242), 雷帕霉素激酶机制靶点抑制剂；含 PAS 结构域的丝氨酸/苏氨酸激酶抑制剂
有货
为什么选择此级别
Moligand™ 级 ，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
-80℃储存。特低温运输 。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
Torkinib (PP242)是一种选择性的mTOR抑制剂，IC50为8 nM；靶向作用于mTOR复合体，作用于mTOR比作用于PI3Kδ或PI3Kα/β/γ选择性分别高10倍多和100倍。A selective FRAP inhibitor
Information
Torkinib (PP242) Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and
In vitro
PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110α, p110β, p110γ, p110δ, and DNA-PK with IC50 of 1.96 μM, 2.2 μM, 1.27 μM, 0.102 μM, and 0.408 μM, respectively. PP242 displays some inhibitory activity against Ret, PKCα, PKCβ, and JAK2, while exhibits remarkable selectivity against 215 other protein kinases. Unlike rapamycin, PP242 inhibits both mTORC1 and mTORC2. In BT549 cells, PP242 treatment (0.04-10 μM) inhibits the phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 in a dose-dependent manner. PP242 potently inhibits PKCα with IC50 of 49 nM. Low concentrations of PP242 inhibit the phosphorylation of Akt S473 and higher concentrations partially inhibit Akt T308-P in addition to S473-P. As PP242 is a more effective mTORC1 inhibitor than rapamycin, PP242 inhibits the proliferation of primary MEFs, and the phosphorylation of 4EBP1 at T36/45 and S65, more potently than rapamycin. PP242 but not rapamycin potently inhibits cap-dependent translation, by causing a higher level of binding between 4EBP1 and eIF4E than rapamycin. PP242 potently inhibits the proliferation of p190-transformed murine BM, SUP-B15, and K562 cells with GI50 of 12 nM, 90 nM, and 85 nM, respectively. PP242 also inhibits the growth of solid tumor cell lines such as SKOV3, PC3, 786-O, and U87 with GI50 of 0.49 μM, 0.19 μM, 2.13 μM, and 1.57 μM, respectively. PP242 is also more effective than rapamycin in achieving cytoreduction and apoptosis in multiple myeloma (MM) cells.
In vivo
Administration of PP242 is able to completely inhibit the phosphorylation of Akt at S473 and T308 in fat and liver of mice. PP242 only partially inhibits the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the phosphorylation of T308 than S473, despite able to fully inhibit the phosphorylation of 4EBP1 and S6. Oral administration PP242 potently delays the leukemia onset in the mice model, and induces leukemia regression by inhibiting mTORC2 and mTORC1 activation that correlates with loss in cell size. PP242 treatment potently inhibits the growth of 8226 cells in mice.
Cell Data
cell lines：Different tumor cell lines including NCI-H460, MDA-MB231, MES-SA, NCI-H460 PTX, MDA-MB-231 PTX, MES-SA Dx5, and HCT-15.
Concentrations：Dissolved in DMSO, final concentrations ~10 μM
Incubation Time：72 hours
Powder Purity:≥97%
规格
别名
托基尼（PP242）
英文别名
2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Torkinib (PP242)
生化机理
Torkinib（PP242）是一种选择性mTOR抑制剂，在无细胞实验中的IC50为8 nM；靶向两种mTOR复合物，对mTOR的选择性分别是PI3Kδ或PI3Kα/β/γ的10倍和100倍。托基尼（PP242）可诱导有丝分裂和细胞凋亡。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
雷帕霉素激酶机制靶点抑制剂；含 PAS 结构域的丝氨酸/苏氨酸激酶抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(N3)C=CC(=C4)O)N
分子量
308.34
Reaxy-Rn
11730137
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11730137&ln=
技术文档
高级数据
关联靶点（人）
RET
Tclin
原癌基因酪氨酸蛋白激酶受体 Ret(Proto-oncogene tyrosine-protein kinase receptor Ret)
(2 活性数据)
PIP5K1C
Tchem
磷脂酰肌醇 4-磷酸 5-激酶 1 型γ(Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma)
(1 活性数据)
PRKCE
Tchem
蛋白激酶 C ε 型(Protein kinase C epsilon type)
(1 活性数据)
MAP3K19
Tchem
丝裂原活化蛋白激酶激酶激酶19(Mitogen-activated protein kinase kinase kinase 19)
(1 活性数据)
BMPR1B
Tchem
骨形态发生蛋白受体 1B 型(Bone morphogenetic protein receptor type-1B)
(1 活性数据)
BRSK1
Tchem
丝氨酸/苏氨酸蛋白激酶 BRSK1(Serine/threonine-protein kinase BRSK1)
(1 活性数据)
ACVR2A
Tchem
激活素受体 2A 型(Activin receptor type-2A)
(1 活性数据)
ACVR2B
Tchem
激活素受体 2B 型(Activin receptor type-2B)
(1 活性数据)
ACVR1
Tchem
激活素受体 1 型(Activin receptor type-1)
(1 活性数据)
ACVRL1
Tchem
丝氨酸/苏氨酸蛋白激酶受体 R3(Serine/threonine-protein kinase receptor R3)
(1 活性数据)
JAK2
Tclin
酪氨酸蛋白激酶JAK2(Tyrosine-protein kinase JAK2)
(1 活性数据)
MAP2K5
Tchem
双特异性丝裂原活化蛋白激酶激酶 5(Dual specificity mitogen-activated protein kinase kinase 5)
(1 活性数据)
MTOR
Tclin
丝氨酸/苏氨酸蛋白激酶 mTOR(Serine/threonine-protein kinase mTOR)
(6 活性数据)
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 H2426080 |
分析证书 | T409136 |
技术文档和文章
溶液计算器
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