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CO-1686(AVL-301),EGFR抑制剂, 表皮生长因子受体 erbB1 抑制剂

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货号 (SKU) 包装规格 是否现货 价格 数量
C124905-5mg
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C124905-10mg
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C124905-50mg
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C124905-100mg
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Egfr (255) epidermal growth factor receptor Inhibitor (73) JAK/STAT Signaling (508) Protein Tyrosine Kinase/RTK (1319) Receptor Tyrosine Kinase (2808)
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基本描述

英文别名 NSC779405 | NSC-779405 | s7284 | NCGC00386293-08 | SB16488 | HUFOZJXAKZVRNJ-UHFFFAOYSA-N | CO1686 | CO-1686 | DB11907 | DTXSID801025958 | Tox21_111814 | CO-1686(Rociletinib) | EINECS 233-234-9 | HMS3653G08 | SCHEMBL4177736 | Rociletinib (CO-1686, AVL-301)
规格或纯度 Moligand™, ≥99%
英文名称 CO-1686 (AVL-301)
生化机理 说明：IC50 值：21.5±1.7 nM（表皮生长因子受体 L858R/T790M）；303.3 ± 26.7 nM（表皮生长因子受体 WT）[1]CO-1686 是一种新型、不可逆、口服给药的激酶抑制剂，它专门针对包括 T790M 在内的表皮生长因子受体突变形式，同时对野生型（WT）受体的活性极低：CO-1686 是表皮生长因子受体 L858R/T790M 激酶的强效抑制剂（kinact/Ki = (2.41 ± 0.30) x 105 M-1s-1），其选择性约为 WT 表皮生长因子受体（kinactt/Ki = (1.12 ± 0.14) x 104 M-1s-1）的 22 倍。CO-1686 能有效抑制突变型 EGFR NSCLC 细胞的增殖，其 GI50 值为 7 - 32 nM。相比之下，由扩增的 WT 表皮生长因子受体（19）驱动的表皮样细胞系 A431 细胞的 GI50 值为 547 nM。两种存在 N 或 KRAS 突变的表达 WT 表皮生长因子受体的细胞系（NCI-H1299 和 NCI-H358）分别在 4275 和 1806 nM 的浓度下受到 CO-1686 的抑制 [1]。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 表皮生长因子受体 erbB1 抑制剂
产品介绍

CO-1686 (AVL-301)是一种不可逆的，突变选择性的EGFR抑制剂，作用于EGFRL858R/T790M和EGFRWT， Ki分别为21.5 nM和303.3 nM。Phase 2。

CO-1686 is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT, respectively. Phase 2.
纯度 ≥99%

产品属性

ALogP 4

关联靶点（人）

EGFR Tclin 表皮生长因子受体(Epidermal growth factor receptor) (30 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TOP2A Tclin DNA topoisomerase II alpha (6317 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IMPDH2 Tclin Inosine-5'-monophosphate dehydrogenase 2 (1326 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DCK Tchem Deoxycytidine kinase (530 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NQO2 Tchem Quinone reductase 2 (885 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADK Tchem Adenosine kinase (1481 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AK2 Tbio Adenylate kinase 2 (264 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKACB Tchem cAMP-dependent protein kinase beta-1 catalytic subunit (589 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAP2K6 Tchem Dual specificity mitogen-activated protein kinase kinase 6 (1284 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MYLK Tchem Myosin light chain kinase, smooth muscle (1267 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSNK1G1 Tchem Casein kinase I gamma 1 (2496 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
STK3 Tchem Serine/threonine-protein kinase MST2 (3069 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKAG1 Tchem AMP-activated protein kinase, gamma-1 subunit (254 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (650 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAP2K3 Tchem Dual specificity mitogen-activated protein kinase kinase 3 (632 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CDK6 Tclin Cyclin-dependent kinase 6 (1724 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKAG2 Tchem AMP-activated protein kinase, gamma-2 subunit (243 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AKT2 Tchem Serine/threonine-protein kinase AKT2 (4301 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AKT3 Tchem Serine/threonine-protein kinase AKT3 (3157 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GRK2 Tchem G-protein coupled receptor kinase 2 (1019 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PYGB Tchem Brain glycogen phosphorylase (474 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA4 Tchem Ribosomal protein S6 kinase alpha 4 (2104 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ROCK1 Tclin Rho-associated protein kinase 1 (4723 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PKN2 Tchem Protein kinase N2 (1991 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKD3 Tchem Protein kinase C nu (2315 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKCI Tchem Protein kinase C iota (2821 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SYK Tclin Tyrosine-protein kinase SYK (7372 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK1 Tclin Tyrosine-protein kinase JAK1 (8569 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA6 Tchem Ribosomal protein S6 kinase alpha 6 (2027 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PFKP Tbio Phosphofructokinase platelet type (224 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSNK1E Tclin Casein kinase I epsilon (1412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CAMK4 Tbio CaM kinase IV (2116 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GSK3A Tclin Glycogen synthase kinase-3 alpha (3764 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKG1 Tchem cGMP-dependent protein kinase 1 beta (2814 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase 2 (1262 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）

Cdk4 Cyclin-dependent kinase 4 (3 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pygl Liver glycogen phosphorylase (81 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Prkcd Protein kinase C delta (192 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Prkcb Protein kinase C beta (2 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
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
Camk2g CaM kinase II gamma (1 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Tec Tyrosine-protein kinase TEC (25 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
BaF3 (4657 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
COS-7 (515 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AIRC Multifunctional protein ADE2 (8 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
Septin9 Septin-9 (1 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Acadvl Very long-chain specific acyl-CoA dehydrogenase, mitochondrial (1 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 504771546
分子类型 小分子
IIUPAC Name N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
INCHI 1S/C27H28F3N7O3/c1-4-24(39)32-18-6-5-7-19(14-18)33-25-21(27(28,29)30)16-31-26(35-25)34-22-9-8-20(15-23(22)40-3)37-12-10-36(11-13-37)17(2)38/h4-9,14-16H,1,10-13H2,2-3H3,(H,32,39)(H2,31,33,34,35)
InChi Key HUFOZJXAKZVRNJ-UHFFFAOYSA-N
Smiles CC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC
Isomeric SMILES CC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC
分子量 555.55
Reaxy-Rn 23999130
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23999130&ln=

化学和物理性质

溶解性 DMSO 100 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
分子量 555.600 g/mol
XLogP3 4.000
氢键供体数Hydrogen Bond Donor Count 3
氢键受体数Hydrogen Bond Acceptor Count 11
可旋转键计数Rotatable Bond Count 8
精确质量Exact Mass 555.221 Da
单同位素质量Monoisotopic Mass 555.221 Da
拓扑极表面积Topological Polar Surface Area 112.000 Ų
重原子数Heavy Atom Count 40
形式电荷Formal Charge 0
复杂度Complexity 871.000
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 1

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批号(Lot Number) 证书类型 货号
K2120355 分析证书 C124905
K2120357 分析证书 C124905
A1509016 分析证书 C124905

引用文献

1. Yu HA, Riely GJ.  (2013)  Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in lung cancers..  J Natl Compr Canc Netw,  11  (2): (161-9).  [PMID:23411383]
2. Walter AO, Sjin RT, Haringsma HJ, Ohashi K, Sun J, Lee K, Dubrovskiy A, Labenski M, Zhu Z, Wang Z et al..  (2013)  Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC..  Cancer Discov,  3  (12): (1404-15).  [PMID:24065731]
3. Ou SH, Soo RA.  (2015)  Dacomitinib in lung cancer: a "lost generation" EGFR tyrosine-kinase inhibitor from a bygone era?.  Drug Des Devel Ther,  9  (5641-53).  [PMID:26508839]

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