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leniolisib (CDZ 173), PI3 激酶 p110-delta 亚基抑制剂

p110δ 选择性抑制剂
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货号 (SKU) 包装规格 是否现货 价格 数量
L414153-1mg
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L414153-5mg
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L414153-10mg
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L414153-25mg
 25mg 期货 Stock Image
L414153-50mg
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L414153-100mg
 100mg 现货 Stock Image
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查看相关系列
phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit alpha Inhibitor (76) phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit delta Inhibitor (71) PI3K (243) PI3K/Akt/mTOR (764)
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基本描述

别名 莱尼奥利西布 (CDZ 173)
英文别名 Q27282602 | US8653092, 67 | Example 67 [WO2012004299] | Leniolisib | Leniolisib; CDZ173 | DC22326 | GTPL9424 | Leniolisib (USAN/INN) | LENIOLISIB [WHO-DD] | s8752 | (S)-1-(3-((6-(6-methoxy-5-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]p
规格或纯度 Moligand™, ≥99%
英文名称 leniolisib (CDZ 173)
生化机理 莱尼利西布（CDZ 173）是一种强效的 PI3Kδ 选择性抑制剂，对 PI3Kα、PI3Kβ、PI3Kγ 和 PI3Kδ 的生化 IC50 值分别为 0.244、0.424、2.23 和 0.011 μM。
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 PI3 激酶 p110-delta 亚基抑制剂
产品介绍


Information

Leniolisib (CDZ 173) is a potentPI3Kδselective inhibitor withbiochemical IC50 valuesof 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.


Targets

PI3Kδ (Cell-free assay); PI3Kα (Cell-free assay); PI3Kβ (Cell-free assay); DNA-PK ; DNA-PK (Cell-free assay) 31052,0.011 μM; 0.244 μM; 0.424


In vitro

CDZ173 inhibits a large spectrum of immune cell functions, as demonstrated in B and T cells, neutrophils, monocytes, basophils, plasmocytoid dendritic cells, and mast cells. CDZ173 showed no activity up to the highest test concentration when tested against CYP isoform assays (3A3, 2D9, 2D6, 2C9), a panel of ion channels (including hERG) and a protease panel. In a panel of 50 safety related targets (GPCRs, ion channels, transporters), CDZ173 only showed measurable activity for hPDE4D (IC50 = 4.7 μM) and 5HT2B (IC50 = 7.7 μM).


In vivo

CDZ173 inhibits B cell activation in rats and monkeys in a concentration- and time-dependent manner. After prophylactic or therapeutic dosing, CDZ173 potently inhibited antigen-specific antibody production and reduced disease symptoms in a rat collagen-induced arthritis model. CDZ173 is absorbed very quickly across species as can be seen by an early Tmax of the oral profiles. Whereas clearance is low to moderate in rats and monkeys, it was found that clearance in dogs is very low resulting in a very high exposure in blood. Plasma protein binding in dogs is very high (>99%) and the distribution of the compound is restricted into tissue (Vss = 0.3 L/kg).
纯度 ≥99%

产品属性

IC50 PI3Kδ, IC50: 0.011 μM
ALogP 2.65
hba_count 5
HBD Count 1
Rotatable Bond 6

关联靶点（人）

PIK3CA Tclin 磷脂酰肌醇 4,5-双磷酸 3-激酶催化亚基 α 异构体(Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform) (1 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)
PIK3CD Tclin 磷脂酰肌醇 4,5-双磷酸 3-激酶催化亚基 delta 异构体(Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform) (3 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
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKDC Tchem DNA-dependent protein kinase (1929 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
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
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
PIK3CD Tclin PI3-kinase p110-delta subunit (6699 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MTOR Tclin Serine/threonine-protein kinase mTOR (13850 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PIK3CG Tclin PI3-kinase p110-gamma subunit (5411 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PI4KB Tchem PI4-kinase beta subunit (1593 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PIK3CB Tchem PI3-kinase p110-beta subunit (4044 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TP53 Tchem Cellular tumor antigen p53 (48468 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
U2OS (164939 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SUD4 (402 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PIK3C3 Tchem Phosphatidylinositol 3-kinase catalytic subunit type 3 (535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DOHH-2 (352 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HEK-293T (167025 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JeKo-1 (376 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pfeiffer (261 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SU-DHL-6 (338 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rec1 (136 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）

PIK3CA PI3-kinase p110-alpha subunit (51 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pde4d Phosphodiesterase 4D (4 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
Fgfr3 Fibroblast growth factor receptor 3 (21 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
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
Pik3cg Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (160 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pik3cd Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (89 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 504771611
分子类型 小分子
IIUPAC Name 1-[(3S)-3-[[6-[6-methoxy-5-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]pyrrolidin-1-yl]propan-1-one
INCHI 1S/C21H25F3N6O2/c1-3-18(31)30-6-4-13(10-30)28-19-15-11-29(7-5-17(15)26-12-27-19)14-8-16(21(22,23)24)20(32-2)25-9-14/h8-9,12-13H,3-7,10-11H2,1-2H3,(H,26,27,28)/t13-/m0/s1
InChi Key MWKYMZXCGYXLPL-ZDUSSCGKSA-N
Smiles CCC(=O)N1CCC(C1)NC2=NC=NC3=C2CN(CC3)C4=CC(=C(N=C4)OC)C(F)(F)F
Isomeric SMILES CCC(=O)N1CC[C@@H](C1)NC2=NC=NC3=C2CN(CC3)C4=CC(=C(N=C4)OC)C(F)(F)F
分子量 450.46
Reaxy-Rn 26178216
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26178216&ln=

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 90 mg/mL (199.79 mM); Ethanol: 13 mg/mL (28.85 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 90
DMSO(mM) Max Solubility 199.795764329796
Water(mg / mL) Max Solubility ＜1
分子量 450.500 g/mol
XLogP3 2.500
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 10
可旋转键计数Rotatable Bond Count 5
精确质量Exact Mass 450.199 Da
单同位素质量Monoisotopic Mass 450.199 Da
拓扑极表面积Topological Polar Surface Area 83.500 Ų
重原子数Heavy Atom Count 32
形式电荷Formal Charge 0
复杂度Complexity 654.000
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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找到4个结果

批号(Lot Number) 证书类型 货号
H2223377 分析证书 L414153
H2223462 分析证书 L414153
H2223463 分析证书 L414153
H2223464 分析证书 L414153

引用文献

1. Lucas CL, Kuehn HS, Zhao F, Niemela JE, Deenick EK, Palendira U, Avery DT, Moens L, Cannons JL, Biancalana M et al..  (2014)  Dominant-activating germline mutations in the gene encoding the PI(3)K catalytic subunit p110δ result in T cell senescence and human immunodeficiency..  Nat Immunol,  15  (1): (88-97).  [PMID:24165795]
2. Wentink M, Dalm V, Lankester AC, van Schouwenburg PA, Schölvinck L, Kalina T, Zachova R, Sediva A, Lambeck A, Pico-Knijnenburg I et al..  (2017)  Genetic defects in PI3Kδ affect B-cell differentiation and maturation leading to hypogammaglobulineamia and recurrent infections..  Clin Immunol,  176  (77-86).  [PMID:28104464]
3. Hoegenauer K, Soldermann N, Zécri F, Strang RS, Graveleau N, Wolf RM, Cooke NG, Smith AB, Hollingworth GJ, Blanz J et al..  (2017)  Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors..  ACS Med Chem Lett,  8  (9): (975-980).  [PMID:28947947]
4. Rao VK, Webster S, Dalm VASH, Šedivá A, van Hagen PM, Holland S, Rosenzweig SD, Christ AD, Sloth B, Cabanski M et al..  (2017)  Effective "activated PI3Kδ syndrome"-targeted therapy with the PI3Kδ inhibitor leniolisib..  Blood,  130  (21): (2307-2316).  [PMID:28972011]

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