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名称

MK-2206 2HCl, AKT 丝氨酸/苏氨酸激酶 1 的变构调节剂；AKT 丝氨酸/苏氨酸激酶 2 的变构调节剂；AKT 丝氨酸/苏氨酸激酶 3 的变构调节剂

分子类型

未知

英文别名

1032350-13-2 | MFCD14584463 | 4-[[(2S,4R)-5-Ethoxy-4-methyl-5-oxo-1-(4-phenylphenyl)pentan-2-yl]amino]-4-oxobutanoic acid calcium salt | AC-28437 | J-000912 | MK 2206 dihydrochloride | 8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]nap

英文名称

MK-2206 2HCl

货号

M129684-100mg

包装规格

100mg

级别

Moligand™

浓度

≥98%

储存温度

-20°C储存,充氩

运输条件

超低温冰袋运输

敏感性

对湿度敏感

产品介绍

MK-2206 2HCl是一种高度选择性的Akt1/2/3抑制剂，IC50分别为8 nM/12 nM/65 nM；对250种其他蛋白激酶没有抑制活性。A highly selective pan-Akt inhibitor activated by the pleckstrin homology domain MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. A highly selective pan-Akt inhibitor activated by the pleckstrin homology domain

生化机理

MK-2206 2HCl 是 Akt1、Akt2 和 Akt3 的高选择性抑制剂，IC50 值分别为 8 nM、12 nM 和 65 nM。MK-2206 是一种异构抑制剂，由 pleckstrin 同源结构域激活。MK-2206 可抑制 Akt T308 和 S473 的自动磷酸化。MK-2206 还能阻止 Akt 介导的下游信号分子磷酸化，包括 TSC2、PRAS40 和核糖体 S6 蛋白。在肺癌 NCI-H460 或卵巢癌 A2780 肿瘤细胞中，MK-2206 还能与厄洛替尼或拉帕替尼等细胞毒性药物联用，产生协同效应。

应用

A highly selective pan-Akt inhibitor activated by the pleckstrin homology domain

CAS号

1032350-13-2

分子式

C25H21N5O·2HCl

分子量

480.39 g/mol

EC号

PubChem SID: 504770874

PubChem编号

46930998

Isomeric SMILES

C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl

IIUPAC Name

8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride

INCHI

1S/C25H21N5O.2ClH/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31;;/h1-3,5-11,14-15H,4,12-13,26H2,(H,29,31);2*1H

InChi Key

HWUHTJIKQZZBRA-UHFFFAOYSA-N

Smiles

C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl

PubChem CID

46930998

PubChem SID

504770874

溶解性

Soluble in DMSO (≥92 mg/ml), water (≥92 mg/ml), ethanol (≥1.8 mg/ml), and methanol.

熔点

>225°C

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

479.128 Da

单同位素质量Monoisotopic Mass

479.128 Da

拓扑极表面积Topological Polar Surface Area

83.600 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

760.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

作用类型

变构调节剂

作用机制

AKT 丝氨酸/苏氨酸激酶 1 的变构调节剂；AKT 丝氨酸/苏氨酸激酶 2 的变构调节剂；AKT 丝氨酸/苏氨酸激酶 3 的变构调节剂

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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