UT-155

未知

UT-155

U648905-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

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)

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。

2031161-35-8

C20H15F4N3O2

405.35 g/mol

122640156

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

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

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

CFSAYQVTXBMPRF-IBGZPJMESA-N

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

122640156

DMSO : ≥ 130 mg/mL (320.71 mM)

2

7

4

405.11 Da

405.11 Da

78.100 Ų

29

0

664.000

0

1

3.100