[2]. Ponnusamy S, et al. Novel Selective Agents for the Degradation of Androgen Receptor Variants to Treat Castration-Resistant Prostate Cancer. Cancer Res. 2017 Nov 15;77(22):6282-6298.
UT-155 是一种选择性的、有效的雄激素受体 (AR) 拮抗剂,与 AR-LBD 结合的 Ki 值为 267 nM。
UT-155 Chemical Structure
CAS No. : 2031161-35-8
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10 mM * 1 mL in DMSO
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UT-155 相关产品
•相关化合物库:
Bioactive Compound Library Plus
Anti-Cancer Compound Library
Transcription Factor Targeted Library
生物活性
UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
IC50 & Target
Ki: 267 nM (AR-LBD)[1].
体外研究 (In Vitro)
UT-155 binds to the AR-LBD at Ki 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[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (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[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
405.35
Formula
C20H15F4N3O2
CAS 号
2031161-35-8
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Ponnusamy S, et al. Novel Selective Agents for the Degradation of Androgen Receptor Variants to Treat Castration-Resistant Prostate Cancer. Cancer Res. 2017 Nov 15;77(22):6282-6298.
UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy[1][2].
UT-34 (3-10 µM; 24 hours; LNCaP cells) treatment inhibits the expression of PSA and FKBP5 and growth of LNCaP cells starting from 100 nM with maximum effect observed at 10 μM[1]. UT-34 (0.1-10 µM; 24 hours; LNCaP cells) treatment results in a reduction of AR levels at 1000 nM in LNCaP cells[1]. Treatment of ZR-75-1 cells maintained in serum-containing growth medium with UT-34 results in downregulation of AR protein levels, but not estrogen receptor (ER) or progesterone receptor (PR) levels. Furthermore, in MDA-MB-453 breast cancer cells that express AR and glucocorticoid receptor (GR), UT-34 induces the downregulation of AR, but not GR[1]. UT-34 is an effective degrader of both AR and AR-V7. LNCaP-ARV7 cells are treated for 24 hours in the presence of 0.1 nM R1881 or 10 ng/mL Doxycycline. Doxycycline induces the expression of EDN2, which is inhibited by UT-34, while UT-34 inhibits the expression of R1881-induced FKBP5 gene expression[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
LNCaP cells
Concentration:
3 µM, 10 µM
Incubation Time:
24 hours
Result:
Inhibited the expression of PSA and FKBP5 and growth of LNCaP cells starting from 100 nM with maximum effect observed at 10 μM.
Western Blot Analysis[1]
Cell Line:
LNCaP cells
Concentration:
0.1 µM, 1 µM, 10 µM
Incubation Time:
24 hours
Result:
Resulted in a reduction of AR levels at 1000 nM.
体内研究 (In Vivo)
UT-34 (20-40 mg/kg; oral administration; daily; for 14 days; NSG mice) at 20 and 40 mg/kg reduces the seminal vesicle weight by 10%-20% and 50%-60 %, respectively[1]. UT-34 inhibits androgen-dependent tissues such as prostate and seminal vesicles in rats, and the growth of Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenografts. UT-34 also induces tumor regression in intact immunocompromised rats[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Non obese diabetic/severe combined immunodeficiency Gamma (NSG) mice injected with MR49F cells[1]
Dosage:
20 mg/kg or 40 mg/kg
Administration:
Oral administration; daily; for 14 days
Result:
Reduced the seminal vesicle weight.
分子量
356.27
Formula
C15H12F4N4O2
CAS 号
2168525-92-4
运输条件
Room temperature in continental US; may vary elsewhere.