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| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| I414189-1mg |
1mg |
现货 ![]() |
| |
| I414189-5mg |
5mg |
现货 ![]() |
| |
| I414189-10mg |
10mg |
现货 ![]() |
| |
| I414189-25mg |
25mg |
现货 ![]() |
| |
| I414189-50mg |
50mg |
现货 ![]() |
|
| 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% |
| 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 |
| 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 |
¥3,999.90