2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Androgen Receptor HSP
  4. Androgen receptor degrader-6

Androgen receptor degrader-6 是一种可穿透血脑屏障的 AR 降解剂。Androgen receptor degrader-6 可抑制 HSP27 的伴侣活性，并破坏 HSP27-AR 复合物。Androgen receptor degrader-6 可促进野生型及突变型 AR 降解，降低 AR 蛋白水平，并抑制胶质母细胞瘤细胞生长。Androgen receptor degrader-6 可用于胶质母细胞瘤的研究。

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Androgen receptor degrader-6

Androgen receptor degrader-6 Chemical Structure

CAS No. : 1372688-55-5

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Androgen receptor degrader-6 相关抗体

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Androgen receptor degrader-6 is a blood-brain barrier-permeable AR degrader. Androgen receptor degrader-6 inhibits the chaperone activity of HSP27 and disrupts the HSP27-AR complex. Androgen receptor degrader-6 promotes the degradation of wild-type and mutant AR, reduces AR protein levels, and inhibits the growth of glioblastoma cells. Androgen receptor degrader-6 can be used in glioblastoma research[1].

体外研究
(In Vitro)

Androgen receptor degrader-6 (compound A) (48 h) 可抑制 T98G、U87 和 DI318 胶质母细胞瘤 (GBM) 细胞的生长[1]。
Androgen receptor degrader-6 (0.5-2 μM) 可剂量依赖性降低 U87、T98G 和 DI318 胶质母细胞瘤 (GBM) 细胞中野生型 AR 蛋白水平，并降低 T98G GBM 细胞中突变型 AR-V7 蛋白水平[1]。
Androgen receptor degrader-6 (0.5-1 μM; 30 min heat shock at 42 °C) 可抑制 T98G 和 U87 胶质母细胞瘤 (GBM) 细胞中 Ser78 位点的 HSP27 磷酸化，但对 Ser82 位点的磷酸化无影响[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Androgen receptor degrader-6 相关抗体:

Cell Viability Assay[1]

Cell Line: AR-overexpressing GBM cell lines T98G, U87; patient-derived GBM cell line DI318
Concentration: /
Incubation Time: 48 h
Result: Inhibited T98G cell growth with an IC50 of 240 nM.
Inhibited U87 cell growth with an IC50 of 850 nM.
Inhibited DI318 cell growth with an IC50 of 2.88 μM.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-24 AUC0-∞ T1/2
Mice[1] 20 (Plasma) mg/kg i.p. 18.15 μg/mL 9.27 μg·h/mL 9.68 μg·h/mL 3.11 h
Mice[1] 20 (Brain) mg/kg i.p. 6.68 μg/g 4.90 μg·h/g 5.01 μg·h/g /
体内研究
(In Vivo)

Androgen receptor degrader-6 (20 mg/kg; 腹腔注射; 每周 3 次，持续 14 天) 可显著抑制裸鼠皮下胶质母细胞瘤异种移植物的生长，并降低肿瘤中 AR 蛋白水平，且未观察到全身毒性[1]。
Androgen receptor degrader-6 (200 mg/kg; 腹腔注射; 每日一次；连续 10 天) 在 C57BL/6 小鼠中未观察到毒性，小鼠体重稳定、血液学指标正常且器官组织学形态无异常[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NCRNU nude mice (male, 5-6 weeks old, n=4 per group, subcutaneous glioblastoma xenograft model)[1]
Dosage: 20 mg/kg
Administration: i.p.; three times per week; 14 days
Result: Significantly reduced xenograft tumor volume compared to vehicle control.
Reduced tumor weight compared to vehicle control.
Significantly reduced AR protein expression in tumor tissues compared to vehicle control.
Showed no significant change in mouse body weight relative to vehicle control.
分子量

396.41

Formula

C17H20N2O7S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Androgen receptor degrader-6 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Androgen receptor degrader-61372688-55-5Androgen receptor degrader6Androgen receptor degrader 6Androgen ReceptorHSPHeat shock proteinsHSP27DI318T98Gandrogen receptorU87AR-V7nude miceSer78 phosphorylationblood-brain barrierglioblastomaInhibitorinhibitorinhibit

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