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UC-514321

    级别和纯度:
  • ≥98%
  • CAS编号: 299420-83-0
  • 分子式: C26H35NO5
  • 分子量: 441.56
  • PubChem编号: 339892
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库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
U647255-5mg
5mg 期货 Stock Image
U647255-10mg
10mg 期货 Stock Image
U647255-50mg
50mg 期货 Stock Image

基本描述

规格或纯度 ≥98%
英文名称 UC-514321
生化机理 UC-514321 是 NSC370284 的结构类似物,具有更高的活性,直接靶向 STAT3/5,抑制 TET1 的表达,但不抑制 TET2 或 TET3。UC-514321 在体外和体内都有治疗急性髓性白血病(AML)的潜力,而且毒性低。
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity

In Vitro

UC-514321 increases apoptosis in AML cells not in normal HSPCs. UC-514321 (0-500 nM, 48 h) inhibits AML cells viability TET1-signaling dependently. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MONOMAC-6, THP-1, KOCL-48, KASUMI-1, ML-2, and NB4 cells. Concentration: 0-500 nM. Incubation Time: 48 hours. Result: Most significantly repressed MONOMAC-6 cell viability. Showed no inhibitory effect on the viability of TET1-low AML. RT-PCRCell Line: MONOMAC-6 cells. Concentration: 0-500 nM. Incubation Time: 48 hours. Result: Functioned as TET1-transcription inhibitors in TET1-high AMLs and their anti-leukemic effects are TET1-dependent.

In Vivo

UC-514321 (2.5 mg/kg, ip, once per day, for 10 days) exhibits more potent anti-tumor activity than NSC370284 in AML mice models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MLL-AF9-AML mice and AE9a-AML model . Dosage: 2.5 mg/kg. Administration: IP., once per day, for 10 days. Result: Showed an improved therapeutic effect in AML mouse models in vivo. Prolonged the median survival over three fold.

Form:Solid

IC50& Target:STAT3 STAT5 TET1

纯度 ≥98%

名称和识别符

IIUPAC Name 6-[(3,5-ditert-butyl-4-hydroxyphenyl)-morpholin-4-ylmethyl]-1,3-benzodioxol-5-ol
INCHI 1S/C26H35NO5/c1-25(2,3)18-11-16(12-19(24(18)29)26(4,5)6)23(27-7-9-30-10-8-27)17-13-21-22(14-20(17)28)32-15-31-21/h11-14,23,28-29H,7-10,15H2,1-6H3
InChi Key XNARHFDDQALZPZ-UHFFFAOYSA-N
Smiles CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)C(C2=CC3=C(C=C2O)OCO3)N4CCOCC4
Isomeric SMILES CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)C(C2=CC3=C(C=C2O)OCO3)N4CCOCC4
PubChem CID 339892
NSC Number 368258
分子量 441.56

化学和物理性质

溶解性 Ethanol : 50 mg/mL (113.23 mM; Need ultrasonic) DMSO : 25 mg/mL (56.62 mM; Need ultrasonic)
分子量 441.600 g/mol
XLogP3 5.500
氢键供体数Hydrogen Bond Donor Count 2
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 5
精确质量Exact Mass 441.252 Da
单同位素质量Monoisotopic Mass 441.252 Da
拓扑极表面积Topological Polar Surface Area 71.400 Ų
重原子数Heavy Atom Count 32
形式电荷Formal Charge 0
复杂度Complexity 599.000
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 1
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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