ABBV-744

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ABBV-744  纯度: 99.97%

ABBV-744 是一种首创，具有口服活性和选择性的 BET 家族蛋白 BDII 结构域 (BDII domain)，对 BRD2、BRD3、BRD4 和 BRDT 的 IC50 值为 4~18 nM。ABBV-744 主要由 CYP3A4 代谢，具有类似药物的特性，可用于研究其抗肿瘤功效和耐受性。

ABBV-744

ABBV-744 Chemical Structure

CAS No. : 2138861-99-9

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10 mM * 1 mL in DMSO ￥1650 In-stock
2 mg ￥900 In-stock
5 mg ￥1600 In-stock
10 mg ￥2600 In-stock
25 mg ￥5200 In-stock
50 mg ￥8400 In-stock
100 mg ￥13280 In-stock
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ABBV-744 相关产品

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生物活性

ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with drug-like properties enable the investigation of its antitumor efficacy and tolerability[1].

IC50 & Target[1]

BRD2 (BD2)

8 nM (IC50)

BRD3 (BD2)

13 nM (IC50)

BRDT (BD2)

18 nM (IC50)

BRD4 (BD2)

4 nM (IC50)

BRD4 (BD2)

3 nM (Kd)

体外研究
(In Vitro)

ABBV-744 (90 nM; 0~24 h; LNCaP cells) downregulates the expression of KLK2 and MYC genes[1].
ABBV-744 (90 nM; 0~72 h; LNCaP cells) induces cell cycle arrest in G1 followed by senescence[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.

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 90 nM
Incubation Time: 0~24 hours
Result: Downregulated the expression of KLK2 and MYC genes.

Cell Cycle Analysis[1]

Cell Line: LNCaP cells
Concentration: 90 nM
Incubation Time: 0~72 hours
Result: Induced cell cycle arrest in G1 followed by senescence.

体内研究
(In Vivo)

ABBV-744 (4.7 mg/kg; oral gavage; 28 days) causes a delay in tumor growth and displays equivalent or better antitumor activity compared with ABBV-075[1].
ABBV-744 (30 mg/kg; 14 days) is able to produce significant antitumor activity. ABBV-744 (30 mg/kg) triggers a reduction in platelets of only 20 %[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: Mice
Dosage: 4.7 mg/kg (Pharmacokinetic Analysis)
Administration: Oral gavage; 28 days
Result: Caused a delay in tumor growth and displayed equivalent or better antitumor activity compared with ABBV-075.
Animal Model: Sprague-Dawley rats
Dosage: 30 mg/kg (Pharmacokinetic Analysis)
Administration: 14 days
Result: Produced significant antitumor activity.

Clinical Trial

分子量

491.55

Formula

C28H30FN3O4
CAS 号

2138861-99-9
运输条件

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

4°C, stored under nitrogen

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

DMSO : 100 mg/mL (203.44 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0344 mL 10.1719 mL 20.3438 mL
5 mM 0.4069 mL 2.0344 mL 4.0688 mL
10 mM 0.2034 mL 1.0172 mL 2.0344 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)。-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: ≥ 2.5 mg/mL (5.09 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.09 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.09 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.09 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.09 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.09 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 4.

    请依序添加每种溶剂： 50% PEG300    50% saline

    Solubility: 2.5 mg/mL (5.09 mM); Suspended solution; Need ultrasonic

  • 5.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2 mg/mL (4.07 mM); Clear solution

  • 6.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2 mg/mL (4.07 mM); Clear solution

*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]. Faivre EJ, et al. Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer. Nature. 2020;578(7794):306-310.

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