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umbralisib (TGR-1202), 酪蛋白激酶 1 epsilon 抑制剂;磷脂酰肌醇-4;5-二磷酸 3-激酶催化亚基 delta 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
U413938-5mg
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U413938-10mg
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U413938-25mg
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U413938-50mg
 50mg 现货 Stock Image
U413938-100mg
 100mg 现货 Stock Image
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Casein Kinase (72) casein kinase 1 epsilon Inhibitor (3) Cell Cycle (7376) Cell Cycle/DNA Damage (2603) phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit delta Inhibitor (71) PI3K (243) PI3K/Akt/mTOR (764) Stem Cell/Wnt (1018)
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基本描述

英文别名 (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one | AKOS025396183 | AS-52257 | 2-((1S)-1-(4-Amino-3-(3-fluoro-4-(1-methylethoxy)phenyl)-1H-pyrazolo(3,4-d)pyrimidin-1-yl)e
规格或纯度 Moligand™, ≥99%
英文名称 umbralisib (TGR-1202)
生化机理 Umbralisib（TGR-1202，Rp-5264）是一种新型的新一代 PI3Kδ 抑制剂，在基于酶和细胞的试验中可抑制 PI3Kδ 的活性，其 IC50 和 EC50 值分别为 22.2 和 24.3 nM。
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 酪蛋白激酶 1 epsilon 抑制剂;磷脂酰肌醇-4;5-二磷酸 3-激酶催化亚基 delta 抑制剂
产品介绍


Information

Umbralisib (TGR-1202, Rp-5264), a novel, next generationPI3Kδinhibitor, inhibits PI3Kδ activity in enzyme and cell based assays withIC50andEC50values of 22.2 & 24.3 nM, respectively.


Targets

PI3Kδ (Cell-free assay) 22.2 nM


In vitro

The compound displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, the compound causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. Treatment of PBMC with RP5264 results initially in a G2/M arrest followed by subsequent increase in the number of Sub G0 cells. Viability assays demonstrate that the compound causes a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells.


In vivo

The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile.


Cell Research(from reference)

Cell lines：Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells 

Incubation Time：96 h 
纯度 ≥99%

产品属性

IC50 PI3Kδ, IC50: 22.2 nM
ALogP 6.393
HBD Count 1
Rotatable Bond 6

关联靶点（人）

CSNK1E Tclin 酪蛋白激酶 I 同工酶 epsilon(Casein kinase I isoform epsilon) (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) (4 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
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
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
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
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
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
U2OS (164939 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
PIK3R1 Tchem PI3-kinase p110-alpha/p85-alpha (2589 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PIK3R1 Tchem PI3K p110 beta/p85 alpha (919 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

关联靶点（其它种属）

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
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
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
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 504772309
分子类型 小分子
IIUPAC Name 2-[(1S)-1-[4-amino-3-(3-fluoro-4-propan-2-yloxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)chromen-4-one
INCHI 1S/C31H24F3N5O3/c1-15(2)41-24-9-7-18(12-22(24)34)27-26-30(35)36-14-37-31(26)39(38-27)16(3)29-25(17-5-4-6-19(32)11-17)28(40)21-13-20(33)8-10-23(21)42-29/h4-16H,1-3H3,(H2,35,36,37)/t16-/m0/s1
InChi Key IUVCFHHAEHNCFT-INIZCTEOSA-N
Smiles CC(C)OC1=C(C=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)C4=C(C(=O)C5=C(O4)C=CC(=C5)F)C6=CC(=CC=C6)F)F
Isomeric SMILES C[C@@H](C1=C(C(=O)C2=C(O1)C=CC(=C2)F)C3=CC(=CC=C3)F)N4C5=NC=NC(=C5C(=N4)C6=CC(=C(C=C6)OC(C)C)F)N
PubChem CID 72950888
分子量 571.55

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 100 mg/mL warmed with 50ºC Water: bath (174.96 mM); Ethanol: 6 mg/mL warmed with 50ºC Water: bath (10.49 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 100
DMSO(mM) Max Solubility 174.9628204
Water(mg / mL) Max Solubility ＜1
分子量 571.500 g/mol
XLogP3 5.800
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 6
精确质量Exact Mass 571.183 Da
单同位素质量Monoisotopic Mass 571.183 Da
拓扑极表面积Topological Polar Surface Area 105.000 Ų
重原子数Heavy Atom Count 42
形式电荷Formal Charge 0
复杂度Complexity 1020.000
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
H2206124 分析证书 U413938
H2206125 分析证书 U413938
H2206126 分析证书 U413938

引用文献

1. Deng C, Lipstein MR, Scotto L, Jirau Serrano XO, Mangone MA, Li S, Vendome J, Hao Y, Xu X, Deng SX et al..  (2017)  Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies..  Blood,  129  (1): (88-99).  [PMID:27784673]
2. Burris 3rd HA, Flinn IW, Patel MR, Fenske TS, Deng C, Brander DM, Gutierrez M, Essell JH, Kuhn JG, Miskin HP et al..  (2018)  Umbralisib, a novel PI3Kδ and casein kinase-1ε inhibitor, in relapsed or refractory chronic lymphocytic leukaemia and lymphoma: an open-label, phase 1, dose-escalation, first-in-human study..  Lancet Oncol,  19  (4): (486-496).  [PMID:29475723]
3. Barrientos JC.  (2018)  Can umbralisib bring PI3Kδ out of the shadows?.  Lancet Oncol,  19  (4): (432-434).  [PMID:29475725]

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