ABBV-744|cas:2138861-99-9|西域试剂

ABBV-744,99.97%

产品编号：Bellancom-112090| CAS NO：2138861-99-9| 分子式：C₂₈H₃₀FN₃O₄| 分子量：491.55

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货号	价格	库存与货期
Bellancom-112090	￥900.00	杭州北京（现货）
Bellancom-112090	￥1600.00	杭州北京（现货）
Bellancom-112090	￥2600.00	杭州北京（现货）
Bellancom-112090	￥5200.00	杭州北京（现货）
Bellancom-112090	￥8400.00	杭州北京（现货）

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ABBV-744

产品介绍

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，具有类似活性分子的特性，可用于研究其抗肿瘤功效和耐受性。

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 agent-like properties enable the investigation of its antitumor efficacy and tolerability.

体外研究

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

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

Western Blot Analysis

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

Cell Cycle Analysis

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.
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 %.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

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