This is a demo store. No orders will be fulfilled.

Uzansertib phosphate

Pim 抑制剂
    级别和纯度:
  • ≥98%
有货

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
I414189-1mg
1mg 现货 Stock Image
I414189-5mg
5mg 现货 Stock Image
I414189-10mg
10mg 现货 Stock Image
I414189-25mg
25mg 现货 Stock Image
I414189-50mg
50mg 现货 Stock Image
查看相关系列
JAK/STAT Signaling (508) Pim (31)

基本描述

别名 磷酸乌赞塞替布
英文别名 INCB053914 phosphate | PIM inhibitor 1 phosphate
规格或纯度 ≥98%
英文名称 Uzansertib phosphate
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

Uzansertib (INCB053914) phosphate 是一种具有口服活性的,ATP 竞争性泛-PIM 激酶抑制剂,对于 PIM1,PIM2 和 PIM3 的 IC50 分别为 0.24 nM,30 nM 和 0.12 nM。Uzansertib phosphate 对多种血液肿瘤细胞系具有广泛的抗增殖活性。

Information

INCB053914 INCB053914 is a novel, ATP-competitive, small molecule, pan-inhibitor of PIM kinases with IC50 values of 0.24 nM, 30 nM and 0.12 nM for PIM1, PIM2 and PIM3 respectively in biochemical assays.


In vitro

INCB053914 potently inhibits the activities of all three PIM isozymes with half maximal inhibitory concentration (IC50) values in the order of PIM1 ≈ PIM3 < PIM2. It is highly selective against a panel of more than 50 kinases (>475-fold selectivity), except for RSK2 for which INCB053914 has modest potency (IC50 = 7.1 μM). No kinase other than Per-Arnt-Sim (PAS) kinase is significantly inhibited by INCB053914 (100 nM). In cell proliferation assays, INCB053914 is active as a single agent in the majority of cell lines derived from different hematological malignancies, including MM, AML, DLBCL, MCL and T-ALL, with IC50 values ranging from 3-300 nM. INCB053914 synergizes with a variety of cytotoxic and targeted agents, reducing the viability of a panel of hematological tumor cell lines.


In vivo

single-agent INCB053914 inhibits Bcl-2-associated death promoter protein phosphorylation and dose-dependently inhibited tumor growth in acute myeloid leukemia and multiple myeloma xenografts. INCB053914 inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) tumors. A pharmacokinetic analysis of INCB053914 plasma concentrations up to 16 hours post oral administration in MOLM-16 and KMS-12-BM tumor-bearing mice suggests dose proportionality.


Cell Research(from reference)

Concentrations:0-1 μM 

Incubation Time:2 h 

纯度 ≥98%

名称和识别符

IIUPAC Name N-[(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide;phosphoric acid
INCHI 1S/C26H26F3N5O3.H3O4P/c1-12-10-34(11-17(30)25(12)36)24-13-5-8-20(35)22(13)31-9-19(24)33-26(37)18-7-6-16(29)23(32-18)21-14(27)3-2-4-15(21)28;1-5(2,3)4/h2-4,6-7,9,12,17,20,25,35-36H,5,8,10-11,30H2,1H3,(H,33,37);(H3,1,2,3,4)/t12-,17+,20+,25+;/m0./s1
InChi Key CYYVLFVRZDZABX-SEDYQSMDSA-N
Smiles CC1CN(CC(C1O)N)C2=C3CCC(C3=NC=C2NC(=O)C4=NC(=C(C=C4)F)C5=C(C=CC=C5F)F)O.OP(=O)(O)O
PubChem CID 126673672
分子量 611.51

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 50 mg/mL (81.76 mM);    
敏感性 对湿度敏感
分子量 611.500 g/mol
XLogP3
氢键供体数Hydrogen Bond Donor Count 7
氢键受体数Hydrogen Bond Acceptor Count 14
可旋转键计数Rotatable Bond Count 4
精确质量Exact Mass 611.176 Da
单同位素质量Monoisotopic Mass 611.176 Da
拓扑极表面积Topological Polar Surface Area 202.000 Ų
重原子数Heavy Atom Count 42
形式电荷Formal Charge 0
复杂度Complexity 853.000
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 4
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 2

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

通过匹配包装上的批号来查找并下载产品的 COA,每批产品都进行了严格的验证,您可放心使用!

找到8个结果

批号(Lot Number) 证书类型 货号
B2426675 分析证书 I414189
B2426681 分析证书 I414189
B2426682 分析证书 I414189
B2426685 分析证书 I414189
B2426686 分析证书 I414189
B2426684 分析证书 I414189
B2426660 分析证书 I414189
B2426668 分析证书 I414189

溶液计算器