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Galeterone (TOK-001)
点击次数：562发布时间：2013/3/22 10:24:46
更新日期：2022/8/19 17:45:40
所 在 地：美洲
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详细内容
Galeterone （TOK-001）
技术数据:
分子量（MW）: 388.55 化学式: C26H32N2O
溶解度: DMSO 24mg/mL Water <1mg/mL Ethanol 40mg/mL 纯度: >99% 稳定性: at -20℃ CAS号: 851983-85-2, 1239339-16-2 （methanesulfonate）, 1239339-18-4 （sulfate）, 1239339-17-3 （HCl）
生物活性
Galeterone （TOK-001, VN/124-1） is a selective CYP17 inhibitor ａnd androgen receptor （AR） antagonist with IC50 of 300 nM ａnd 384 nM, respectively. Galeterone is effective at preventing binding of [3H]-R1881 （methyltrienolone, a stable synthetic androgen） to both the mutant AR （T877A） in LNCaP cells ａnd the wild-type AR in PC-3AR cells. Galeterone potently inhibits the AR-mediated transcription in LNCaP cells transiently transfected with a probasin luciferase reporter construct AARZ-Luc in a concentration-dependent manner. Galeterone inhibits the growth of DHT-stimulated LNCaP ａnd LAPC4 prostate cancer cells with IC50 of <10 μM. Galeterone is very effective at inhibiting the growth of androgen-dependent LAPC4 human prostate tumor xenograft. [1] In the LAPC4 xenograft, Galeterone is a more potent agent in reducing tumor growth than other compounds （VN/85, VN/87, ａnd VN108） ａnd is more effective than castration ａnd casodex. Treatment with Galeterone markedly reduces AR protein levels both in vivo ａnd in vitro. Thus, Galeterone disrupts androgen receptor （AR） signaling via a novel triple mechanism of action （CYP17 inhibition, competitive inhibition, ａnd down-regulation of the AR）. [2] Galeterone also inhibits the growth of androgen-independent prostate cancer cells via induction of the endoplasmic reticulum stress response. Additionally, Galeterone in combination with thapsigargin exhibits synergistic effect in inhibiting PC-3 cell growth. [3] Galeterone in combination with everolimus or gefitinib demonstrates superior synergy for growth inhibition against hormone-refractory prostate cancer cell line （high-passage LNCaP, HP-LNCaP） compared with bicalutamide. [4] Dual inhibition of AR ａnd mTOR with Galeterone ａnd everolimus acts in concert to reduce tumor growth rates in the castration-resistant prostate cancer xenograft model. [5] Galeterone is a superior inhibitor than abiraterone of R1881-induced transcriptional activity of both wild type ａnd mutant AR. [6]
技术数据:
分子量（MW）: 388.55 化学式: C26H32N2O
溶解度: DMSO 24mg/mL Water <1mg/mL Ethanol 40mg/mL 纯度: >99% 稳定性: at -20℃ CAS号: 851983-85-2, 1239339-16-2 （methanesulfonate）, 1239339-18-4 （sulfate）, 1239339-17-3 （HCl）
生物活性
Galeterone （TOK-001, VN/124-1） is a selective CYP17 inhibitor ａnd androgen receptor （AR） antagonist with IC50 of 300 nM ａnd 384 nM, respectively. Galeterone is effective at preventing binding of [3H]-R1881 （methyltrienolone, a stable synthetic androgen） to both the mutant AR （T877A） in LNCaP cells ａnd the wild-type AR in PC-3AR cells. Galeterone potently inhibits the AR-mediated transcription in LNCaP cells transiently transfected with a probasin luciferase reporter construct AARZ-Luc in a concentration-dependent manner. Galeterone inhibits the growth of DHT-stimulated LNCaP ａnd LAPC4 prostate cancer cells with IC50 of <10 μM. Galeterone is very effective at inhibiting the growth of androgen-dependent LAPC4 human prostate tumor xenograft. [1] In the LAPC4 xenograft, Galeterone is a more potent agent in reducing tumor growth than other compounds （VN/85, VN/87, ａnd VN108） ａnd is more effective than castration ａnd casodex. Treatment with Galeterone markedly reduces AR protein levels both in vivo ａnd in vitro. Thus, Galeterone disrupts androgen receptor （AR） signaling via a novel triple mechanism of action （CYP17 inhibition, competitive inhibition, ａnd down-regulation of the AR）. [2] Galeterone also inhibits the growth of androgen-independent prostate cancer cells via induction of the endoplasmic reticulum stress response. Additionally, Galeterone in combination with thapsigargin exhibits synergistic effect in inhibiting PC-3 cell growth. [3] Galeterone in combination with everolimus or gefitinib demonstrates superior synergy for growth inhibition against hormone-refractory prostate cancer cell line （high-passage LNCaP, HP-LNCaP） compared with bicalutamide. [4] Dual inhibition of AR ａnd mTOR with Galeterone ａnd everolimus acts in concert to reduce tumor growth rates in the castration-resistant prostate cancer xenograft model. [5] Galeterone is a superior inhibitor than abiraterone of R1881-induced transcriptional activity of both wild type ａnd mutant AR. [6]
技术数据:
| 分子量（MW）: | 388.55 | |
|---|---|---|
| 化学式: | C26H32N2O | |
| 溶解度: | DMSO 24mg/mL Water <1mg/mL Ethanol 40mg/mL | |
| 纯度: | >99% | |
| 稳定性: | at -20℃ | |
| CAS号: | 851983-85-2, 1239339-16-2 （methanesulfonate）, 1239339-18-4 （sulfate）, 1239339-17-3 （HCl） |
生物活性
Galeterone （TOK-001, VN/124-1） is a selective CYP17 inhibitor ａnd androgen receptor （AR） antagonist with IC50 of 300 nM ａnd 384 nM, respectively. Galeterone is effective at preventing binding of [3H]-R1881 （methyltrienolone, a stable synthetic androgen） to both the mutant AR （T877A） in LNCaP cells ａnd the wild-type AR in PC-3AR cells. Galeterone potently inhibits the AR-mediated transcription in LNCaP cells transiently transfected with a probasin luciferase reporter construct AARZ-Luc in a concentration-dependent manner. Galeterone inhibits the growth of DHT-stimulated LNCaP ａnd LAPC4 prostate cancer cells with IC50 of <10 μM. Galeterone is very effective at inhibiting the growth of androgen-dependent LAPC4 human prostate tumor xenograft. [1] In the LAPC4 xenograft, Galeterone is a more potent agent in reducing tumor growth than other compounds （VN/85, VN/87, ａnd VN108） ａnd is more effective than castration ａnd casodex. Treatment with Galeterone markedly reduces AR protein levels both in vivo ａnd in vitro. Thus, Galeterone disrupts androgen receptor （AR） signaling via a novel triple mechanism of action （CYP17 inhibition, competitive inhibition, ａnd down-regulation of the AR）. [2] Galeterone also inhibits the growth of androgen-independent prostate cancer cells via induction of the endoplasmic reticulum stress response. Additionally, Galeterone in combination with thapsigargin exhibits synergistic effect in inhibiting PC-3 cell growth. [3] Galeterone in combination with everolimus or gefitinib demonstrates superior synergy for growth inhibition against hormone-refractory prostate cancer cell line （high-passage LNCaP, HP-LNCaP） compared with bicalutamide. [4] Dual inhibition of AR ａnd mTOR with Galeterone ａnd everolimus acts in concert to reduce tumor growth rates in the castration-resistant prostate cancer xenograft model. [5] Galeterone is a superior inhibitor than abiraterone of R1881-induced transcriptional activity of both wild type ａnd mutant AR. [6]
