AU-15330

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AU-15330  纯度: 99.57%

AU-15330 是 SWI/SNF ATP 酶亚基 SMARCA2 和 SMARCA4 的蛋白水解靶向嵌合体 (PROTAC) 降解剂。AU-15330 在前列腺癌异种移植模型中诱导有效抑制肿瘤生长，并与 AR 拮抗剂 enzalutamide 协同作用。AU-15330 在去势抵抗性前列腺癌 (CRPC) 模型中诱导疾病缓解而无毒性。

AU-15330

AU-15330 Chemical Structure

CAS No. : 2380274-50-8

规格 价格 是否有货 数量
5 mg ￥6500 In-stock
10 mg ￥10500 In-stock
50 mg   询价  
100 mg   询价  

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AU-15330 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity[1].

IC50 & Target

SMARCA2 and SMARCA4[1]
体内研究
(In Vivo)

AU-15330 (10 and 30 mg/kg; i.v.; 5 days per week for 3 weeks) shows no evident toxicity in immuno-competent mice[1].
AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) leads to potent inhibition of tumour growth, triggering disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals[1].
AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) strongly inhibits the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide[1].
AU-15330 (60 mg/kg with or without 10 mg/kg enzalutamide; i.v.; 3 days per week; p.o.; 5 days per week for 5 weeks) combines with enzalutamide induces significant tumour growth inhibition, causing regression in more than 30% of animals in the modle of CRPC variant of the MDA-PCa-146-12 PDX by tumour implantation into castrated mice[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: Six-week-old male CB17 severe combined immunodeficiency (SCID) mice[1]
Dosage: 10 and 30 mg/kg
Administration: i.v. (5 days per week for 3 weeks)
Result: Showed no evident toxicity in immuno-competent mice.
Animal Model: VCaP castration-resistant tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)[1]
Dosage: 60 mg/kg with or without 10 mg/kg enzalutamide
Administration: i.v. (3 days per week); p.o. (5 days per week for 5 weeks)
Result: Resulted inhibition of tumor growth and triggered disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals.
Animal Model: C4-2B non-castrated tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)[1]
Dosage: 60 mg/kg with or without 30 mg/kg enzalutamide
Administration: i.v. (3 days per week); p.o. (5 days per week for 4 weeks)
Result: Strongly inhibited the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.

分子量

755.93

Formula

C39H49N9O5S
CAS 号

2380274-50-8
运输条件

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

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
溶解性数据
In Vitro: 

DMSO : 140 mg/mL (185.20 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3229 mL 6.6144 mL 13.2287 mL
5 mM 0.2646 mL 1.3229 mL 2.6457 mL
10 mM 0.1323 mL 0.6614 mL 1.3229 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.5 mg/mL (4.63 mM); Clear solution

    此方案可获得 ≥ 3.5 mg/mL (4.63 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 35.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3.5 mg/mL (4.63 mM); Clear solution

    此方案可获得 ≥ 3.5 mg/mL (4.63 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 35.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 3.5 mg/mL (4.63 mM); Clear solution

    此方案可获得 ≥ 3.5 mg/mL (4.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 35.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Xiao L, et al. Targeting SWI/SNF ATPases in enhancer-addicted prostate cancer. Nature. 2022;601(7893):434-439.

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