| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| M421215-1ml |
1ml |
现货  |
|
| 英文别名 | Miransertib3-[3-[4-(1-aminocyclobutyl)phenyl]-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl]-2-Pyridinamine hydrochloride |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Miransertib (ARQ 092) HCl |
| 生化机理 | Miransertib (ARQ 092) HCl 是一种新型、口服生物利用度高的选择性 AKT 通路抑制剂，对晚期实体瘤患者具有可控的安全性。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
Information Miransertib (ARQ 092) HCl is a novel, orally bioavailable and selectiveAKT pathwayinhibitor exhibiting a manageable safety profile among patients with advanced solid tumors. Targets Akt2 (Cell-free assay); Akt1 (Cell-free assay); Akt3 (Cell-free assay) 4.5 nM; 5 nM; 16 nM In vitro ARQ 092 blocks membrane translocation of inactive AKT and even dephosphorylates the membrane-associated active form, thereby perturbing AKT activity. Treatment with 50-500 nM ARQ 092 significantly blocks αMβ2 integrin function in neutrophils and reduces P-selectin exposure and glycoprotein Ib/IX/V-mediated agglutination in platelets. In a large panel of diverse cancer cell lines, ARQ 092 inhibits proliferation across multiple tumor types but are most potent in leukemia, breast, endometrial, and colorectal cancer cell lines. Moreover, inhibition by ARQ 092 is more prevalent in cancer cell lines containing PIK3CA/PIK3R1 mutations compared to those with wt-PIK3CA/PIK3R1 or PTEN mutations. ARQ 092 targets the PI3K/AKT pathway and AKT specifically and reduces phosphorylation of GSK3α and GSK3β in mutation-positive cells. In vivo Short-term oral administration of ARQ 092 or hydroxyurea, a main therapy for sickle cell disease, diminishes heterotypic cell-cell interactions in venules of sickle cell disease mice challenged with TNF-α. ARQ 092 is well tolerated at a continuous daily dose of 60 mg or a dose of 600 mg when administered once a week, for several months. ARQ 092 is likely to inhibit the activity of all AKT isoforms in intravascular cells and thereby attenuates the process of thrombosis and inflammation in SCD patients. ARQ 092 is highly active in a subset of endometrial tumors that harbor PI3K pathway gene mutations. Cell Research(from reference) Cell lines：MDA-MB-453 cells; NCI-H1650 cells; KU-19-19 cells Concentrations：0, 0.012, 0.037, 0.11, 0.33, and 1 μM Incubation Time：2 h |
| IC50 | Akt2, IC50: 4.5 nM |
|---|---|
| ALogP | 4.98 |
| hba_count | 3 |
| HBD Count | 2 |
| Rotatable Bond | 4 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 未知 |
|---|---|
| IIUPAC Name | 3-[3-[4-(1-aminocyclobutyl)phenyl]-5-phenylimidazo[4,5-b]pyridin-2-yl]pyridin-2-amine;hydrochloride |
| INCHI | 1S/C27H24N6.ClH/c28-24-21(8-4-17-30-24)25-32-23-14-13-22(18-6-2-1-3-7-18)31-26(23)33(25)20-11-9-19(10-12-20)27(29)15-5-16-27;/h1-4,6-14,17H,5,15-16,29H2,(H2,28,30);1H |
| InChi Key | DRHSWSSVIKDJME-UHFFFAOYSA-N |
| Smiles | C1CC(C1)(C2=CC=C(C=C2)N3C4=C(C=CC(=N4)C5=CC=CC=C5)N=C3C6=C(N=CC=C6)N)N.Cl |
| Isomeric SMILES | C1CC(C1)(C2=CC=C(C=C2)N3C4=C(C=CC(=N4)C5=CC=CC=C5)N=C3C6=C(N=CC=C6)N)N.Cl |
| 分子量 | 468.98 |
| Reaxy-Rn | 21570993 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21570993&ln= |
| DMSO(mg / mL) Max Solubility | 75 |
|---|---|
| DMSO(mM) Max Solubility | 159.9215318 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 469.000 g/mol |
| XLogP3 | |
| 氢键供体数Hydrogen Bond Donor Count | 3 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 4 |
| 精确质量Exact Mass | 468.183 Da |
| 单同位素质量Monoisotopic Mass | 468.183 Da |
| 拓扑极表面积Topological Polar Surface Area | 95.600 Ų |
| 重原子数Heavy Atom Count | 34 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 653.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 2 |
| 信号词 | Warning |
|---|---|
| 危险声明 |
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害 |
| 预防措施声明 |
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 |
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