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NVP-CGM097

Mdm2抑制剂
COA COA
    级别和纯度:
  • ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
N413861-2mg
 2mg 现货 Stock Image
N413861-5mg
 5mg 现货 Stock Image
N413861-10mg
 10mg 现货 Stock Image
N413861-25mg
 25mg 现货 Stock Image
N413861-50mg
 50mg 现货 Stock Image
N413861-100mg
 100mg 现货 Stock Image
大包装询价 收藏夹 比较  SDS下载  DATASHEET  质量标准
查看相关系列
Amino Acid/Protein Metabolism (4559) Apoptosis (7108) E1/E2/E3 Enzyme (112) Intrinsic Pathway (1438) MDM-2/p53 (109) Metabolic Enzyme/Protease (4889)
main product photo

基本描述

英文别名 AKOS030526402 | BP-10652 | NSC783015 | NSC-783015 | SCHEMBL2391196 | CCG-270337 | Uridine pyrophosphate a-delta-galactopyranosyl ester | BDBM162123 | CGM 097 [WHO-DD] | MFCD28144684 | (1S)-1-(4-chlorophenyl)-6-methoxy-2-[4-(methyl{[trans-4-(4-methyl-3-oxo
规格或纯度 ≥98%
英文名称 NVP-CGM097
生化机理 NVP-CGM097 是一种高效的选择性 MDM2 抑制剂，在 TR-FRET 试验中对 hMDM2 的 Ki 值为 1.3 nM。它能与 Mdm2 蛋白的 p53 结合位点结合，破坏两种蛋白之间的相互作用，从而激活 p53 通路。
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


Information

NVP-CGM097 NVP-CGM097 is a highly potent and selective MDM2 inhibitor with Ki value of 1.3 nM for hMDM2 in TR-FRET assay. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction between both proteins, leading to an activation of the p53 pathway.


Targets

hMDM2 (Cell-free assay) 1.7 nM


In vitro

NVP-CGM097 binding to MDM2 is species dependent. It was shown to be selective for the p53:MDM2 interaction compared to the p53:MDM4 interaction (1176-fold selectivity) and the Ras:Raf interaction (3000-fold selectivity). In addition, NVP-CGM097 showed no significant activity against Bcl-2:Bak, Bcl-2:Bad, Mcl-1:Bak, Mcl-1:NOXA, XIAP:BIR3, and c-IAP:BIR3 protein-protein interactions. NVP-CGM097 was able to significantly redistribute wild-type p53 into the cell nucleus with an IC50 of 0.224 μM, demonstrating its ability to inhibit the p53:MDM2 interaction in living cells. NVP-CGM097 treatment leads to p53 nuclear translocation that results in cell growth inhibition in a p53-dependent manner.


In vivo

After iv administration, the total blood clearance (CL) of NVP-CGM097 was 5 mL/min/kg for mouse, 7 mL/min/kg for rat, 3 mL/min/kg for dog, and 4 mL/min/kg for monkey. On the basis of the respective hepatic blood flows, NVP-CGM097 showed a consistent low total blood CL in all species (5-10% of hepatic blood flow). The apparent terminal half-life (t1/2) was long in rodents and monkey (6-12 h) but was comparatively longer in dogs (20 h). After oral dosing, the compound was well absorbed with Tmax occurring between 1 and 4.5 h in all species tested. The oral bioavailability (%F) was high in mouse, rat, and dog and moderate in monkey. NVP-CGM097 was able to inhibit the interaction between p53 and MDM2 and reactivate the p53 pathway in vivo in a MDM2-amplified SJSA-1 human tumor model. p21 mRNA levels were found to increase concomitantly with levels of compound 1 in tumor-bearing rats dosed at 30 mg/kg. Daily treatment with NVP-CGM097 dose dependently and significantly inhibited SJSA-1 tumor growth in rats.


Cell Research(from reference)

Cell lines：Bon1 cells, NCI-H727 cells, Got1 cells 

Concentrations：0.1 nM-2500 nM 

Incubation Time：48 hrs, 96 hrs, 144 hrs or 216 hrs 
纯度 ≥98%

产品属性

ALogP 6.455
hba_count 4
Rotatable Bond 9

关联靶点（人）

CYP3A4 Tclin Cytochrome P450 3A4 (53859 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
XIAP Tchem Inhibitor of apoptosis protein 3 (3673 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDM2 Tchem p53-binding protein Mdm-2 (4545 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SAOS-2 (672 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HCT-116 (91556 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HepG2 (196354 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BCL2 Tclin Apoptosis regulator Bcl-2 (3787 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MCL1 Tchem Induced myeloid leukemia cell differentiation protein Mcl-1 (3820 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BIRC2 Tchem Baculoviral IAP repeat-containing protein 2 (984 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDM4 Tchem Protein Mdm4 (729 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TP53 Tchem Tumour suppressor p53/oncoprotein Mdm2 (2075 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SJSA-1 (970 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Canis familiaris (36305 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rhesus monkey (3147 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cynomolgus monkey (4946 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasma (328 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Liver microsome (341 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDM2 E3 ubiquitin-protein ligase Mdm2 (2 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504771113
分子类型 小分子
IIUPAC Name (1S)-1-(4-chlorophenyl)-6-methoxy-2-[4-[methyl-[[4-(4-methyl-3-oxopiperazin-1-yl)cyclohexyl]methyl]amino]phenyl]-7-propan-2-yloxy-1,4-dihydroisoquinolin-3-one
INCHI 1S/C38H47ClN4O4/c1-25(2)47-35-22-33-28(20-34(35)46-5)21-36(44)43(38(33)27-8-10-29(39)11-9-27)32-16-14-30(15-17-32)41(4)23-26-6-12-31(13-7-26)42-19-18-40(3)37(45)24-42/h8-11,14-17,20,22,25-26,31,38H,6-7,12-13,18-19,21,23-24H2,1-5H3/t26?,31?,38-/m0/s1
InChi Key CLRSLRWKONPSRQ-CPOWQTMSSA-N
Smiles CC(C)OC1=C(C=C2CC(=O)N(C(C2=C1)C3=CC=C(C=C3)Cl)C4=CC=C(C=C4)N(C)CC5CCC(CC5)N6CCN(C(=O)C6)C)OC
Isomeric SMILES CC(C)OC1=C(C=C2CC(=O)N([C@H](C2=C1)C3=CC=C(C=C3)Cl)C4=CC=C(C=C4)N(C)CC5CCC(CC5)N6CCN(C(=O)C6)C)OC
分子量 659.26
Reaxy-Rn 21801063
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21801063&ln=

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 65 mg/mL (98.59 mM); Ethanol: 65 mg/mL (98.59 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 65
DMSO(mM) Max Solubility 98.59539484
Water(mg / mL) Max Solubility ＜1
分子量 659.300 g/mol
XLogP3 6.500
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 9
精确质量Exact Mass 658.329 Da
单同位素质量Monoisotopic Mass 658.329 Da
拓扑极表面积Topological Polar Surface Area 65.600 Ų
重原子数Heavy Atom Count 47
形式电荷Formal Charge 0
复杂度Complexity 1040.000
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 1
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 1

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批号(Lot Number) 证书类型 货号
G2219851 分析证书 N413861
G2219852 分析证书 N413861
G2219863 分析证书 N413861
G2219864 分析证书 N413861
G2219949 分析证书 N413861
L2412310 分析证书 N413861

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