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名称

UT-155

分子类型

未知

英文名称

UT-155

货号

U648905-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

UT-155 is a selective and potent androgen receptor (AR) antagonist, with a K i of 267 nM for UT-155 binding to AR-LBD. In Vitro UT-155 binds to the AR-LBD at K i of 267 nM. UT-155 potently inhibits the R1881-induced wildtype AR transactivation with 6-10-fold higher potency than enzalutamide. While UT-155 antagonizes both wildtype and mutant ARs comparably, enzalutamide is weaker by two fold with the W742L mutant AR relative to the wild type AR. Treatment of LNCaP cells with UT-155 inhibits 0.1 nM R1881-induced PSA and FKBP5 gene expression between 10 and 100 nM with 5-10-fold better potency than enzalutamide. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Consistent with the anti-proliferative effects in vitro, UT-155 significantly inhibits the growth of 22RV1 xenograft by 53%, while, as expected, enzalutamide has no effect on the growth of the 22RV1 tumors. Tumor weights and PSA and the expression of AR and AR-SV are significantly lower in UT-155-treated animals . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Ki: 267 nM (AR-LBD)

生化机理

UT-155是一种选择性强的雄激素受体（AR）拮抗剂，UT-155与AR-LBD结合的K i为267 nM。

CAS号

2031161-35-8

分子式

C20H15F4N3O2

分子量

405.35 g/mol

PubChem编号

122640156

Isomeric SMILES

C[C@](CN1C=CC2=C1C=CC(=C2)F)(C(=O)NC3=CC(=C(C=C3)C#N)C(F)(F)F)O

IIUPAC Name

(2S)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(5-fluoroindol-1-yl)-2-hydroxy-2-methylpropanamide

INCHI

1S/C20H15F4N3O2/c1-19(29,11-27-7-6-12-8-14(21)3-5-17(12)27)18(28)26-15-4-2-13(10-25)16(9-15)20(22,23)24/h2-9,29H,11H2,1H3,(H,26,28)/t19-/m0/s1

InChi Key

CFSAYQVTXBMPRF-IBGZPJMESA-N

Smiles

CC(CN1C=CC2=C1C=CC(=C2)F)(C(=O)NC3=CC(=C(C=C3)C#N)C(F)(F)F)O

PubChem CID

122640156

溶解性

DMSO : ≥ 130 mg/mL (320.71 mM)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

405.11 Da

单同位素质量Monoisotopic Mass

405.11 Da

拓扑极表面积Topological Polar Surface Area

78.100 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

664.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

3.100

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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