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MK-2206 2HCl

规格或纯度: ≥98%
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M129684-10mg 10mg 现货 Stock Image
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M129684-100mg 100mg 现货 Stock Image
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AKT serine/threonine kinase 1 Allosteric modulator AKT serine/threonine kinase 2 Allosteric modulator AKT serine/threonine kinase 3 Allosteric modulator
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基本描述

规格或纯度 ≥98%
英文名称 MK-2206 2HCl
别名 MK2206
英文别名 MK2206;MK-2206 dihydrochloride;8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride
生化机理 MK-2206 2HCl is a highly selective inhibitor of Akt1, Akt2, and Akt3 with IC50 values of 8 nM, 12 nM and 65 nM, respectively. MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of both Akt T308 and S473. MK-2206 also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins. MK-2206 also shows synergistic responses in combination with cytotoxic agents such as erlotinib or lapatinib in lung NCI-H460 or ovarian A2780 tumor cells
应用 A highly selective pan-Akt inhibitor activated by the pleckstrin homology domain
储存温度 -20°C储存,充氩
运输条件 超低温冰袋运输
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

名称和标识符

IUPAC Name 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride
INCHI 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
Canonical SMILES C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
分子式

C25H21N5O·2HCl
PubChem CID 46930998
分子量 480.39

化学和物理性质

溶解性 Soluble in DMSO (≥92 mg/ml), water (≥92 mg/ml), ethanol (≥1.8 mg/ml), and methanol.
敏感性 对湿度敏感
熔点 >225°C

靶标

Target ID 1479
名称 AKT serine/threonine kinase 1
缩写名 Akt1
家族 Akt (Protein kinase B, PKB) family
别名 Gpcr17
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 480 14q32.33 AKT1 AKT serine/threonine kinase 1
Mouse 2 480 12 61.2 cM Akt1 thymoma viral proto-oncogene 1
Rat 2 480 6q32 Akt1 AKT serine/threonine kinase 1
Ensembl Gene ENSG00000142208 (Hs) , ENSMUSG00000001729 (Mm) , ENSRNOG00000028629 (Rn)
Entrez Gene 11651 (Mm) , 24185 (Rn) , 207 (Hs)
OMIM 164730 (Hs)
Protein GI 15100164 (Rn) , 62241015 (Hs) , 260166608 (Mm)
UniProtKB P31749 (Hs) , P31750 (Mm) , P47196 (Rn)
RefSeq Nucleotide NM_001014431 (Hs) , NM_009652 (Mm) , NM_033230 (Rn)
RefSeq Protein NP_001014431 (Hs) , NP_001159366 (Mm) , NP_033782 (Mm) , NP_150233 (Rn)
Orphanet 281472 (Hs)
CATH/Gene3D 2.30.29.30 (N/A)
ChEMBL Target CHEMBL4282 (Hs) , CHEMBL1075215 (Rn) , CHEMBL5859 (Mm)
Target ID 1480
名称 AKT serine/threonine kinase 2
缩写名 Akt2
家族 Akt (Protein kinase B, PKB) family
别名 Gpcr17
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 481 19q13.2 AKT2 AKT serine/threonine kinase 2
Mouse 2 481 7 15.94 cM Akt2 thymoma viral proto-oncogene 2
Rat 2 481 1q21 Akt2 AKT serine/threonine kinase 2
Ensembl Gene ENSG00000105221 (Hs) , ENSMUSG00000004056 (Mm) , ENSRNOG00000018677 (Rn)
Entrez Gene 11652 (Mm) , 25233 (Rn) , 208 (Hs)
OMIM 164731 (Hs)
Protein GI 8392888 (Rn) , 339895855 (Hs) , 158937315 (Mm)
UniProtKB P31751 (Hs) , P47197 (Rn) , Q60823 (Mm)
RefSeq Nucleotide NM_001243027 (Hs) , NM_007434 (Mm) , NM_017093 (Rn)
RefSeq Protein NP_001103678 (Mm) , NP_001617 (Hs) , NP_031460 (Mm) , NP_058789 (Rn)
Orphanet 201112 (Hs)
CATH/Gene3D 2.30.29.30 (N/A)
ChEMBL Target CHEMBL5382 (Mm) , CHEMBL2431 (Hs)
Target ID 2286
名称 AKT serine/threonine kinase 3
缩写名 AKT3
家族 Akt (Protein kinase B, PKB) family
别名 Gpcr17
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 479 1q43-q44 AKT3 AKT serine/threonine kinase 3
Mouse 2 479 1 H4 Akt3 thymoma viral proto-oncogene 3
Rat 2 479 13q25 Akt3 AKT serine/threonine kinase 3
Entrez Gene 10000 (Hs) , 23797 (Mm) , 29414 (Rn)
UniProtKB Q9Y243 (Hs) , Q9WUA6 (Mm) , Q63484 (Rn)
Ensembl Gene ENSG00000117020 (Hs) , ENSMUSG00000019699 (Mm) , ENSRNOG00000021497 (Rn)
RefSeq Nucleotide NM_005465 (Hs) , NM_011785 (Mm) , NM_031575 (Rn)
RefSeq Protein NP_005456 (Hs) , NP_035915 (Mm) , NP_113763 (Rn)
OMIM 611223 (Hs)
Orphanet 299660 (Hs)
Protein GI 4885549 (Hs) , 190883484 (Mm) , 13928778 (Rn)
CATH/Gene3D 2.30.29.30 (N/A)
ChEMBL Target CHEMBL4816 (Hs)

关联配体

Ligand ID 7945
名称 MK-2206
别名 MK 2206
类别 Synthetic organic
学名 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one
生物活性评价 MK-2206 is able to enhance the antitumor efficacy of standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo .
评价 MK-2206 is an orally bioavailable allosteric inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity .

参考文献

1. Hirai H, Sootome H, Nakatsuru Y, Miyama K, Taguchi S, Tsujioka K, Ueno Y, Hatch H, Majumder PK, Pan BS et al..  (2010)  MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo..  Mol Cancer Ther,  9  (7):  (1956-67).  [PMID:20571069]
2. Liu R, Liu D, Trink E, Bojdani E, Ning G, Xing M.  (2011)  The Akt-specific inhibitor MK2206 selectively inhibits thyroid cancer cells harboring mutations that can activate the PI3K/Akt pathway..  J Clin Endocrinol Metab,  96  (4):  (E577-85).  [PMID:21289267]
3. Lin YH, Chen BY, Lai WT, Wu SF, Guh JH, Cheng AL, Hsu LC.  (2015)  The Akt inhibitor MK-2206 enhances the cytotoxicity of paclitaxel (Taxol) and cisplatin in ovarian cancer cells..  Naunyn Schmiedebergs Arch Pharmacol,  388  (1):  (19-31).  [PMID:25164962]
4. Holland WS, Chinn DC, Lara Jr PN, Gandara DR, Mack PC.  (2015)  Effects of AKT inhibition on HGF-mediated erlotinib resistance in non-small cell lung cancer cell lines..  J Cancer Res Clin Oncol,  141  (4):  (615-26).  [PMID:25323938]

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