DS89002333|cas:2832159-79-0|西域试剂

DS89002333,99.65%

产品编号：Bellancom-150072| CAS NO：2832159-79-0| 分子式：C₂₂H₂₀ClF₂N₃O₃| 分子量：447.86

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-150072		￥5500.00	杭州北京（现货）
Bellancom-150072		￥16800.00	杭州北京（现货）

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DS89002333

产品介绍

DS89002333 是一种口服有效的强效 PRKACA 抑制剂，其 IC₅₀ 值为 0.3 nM。DS89002333 在表达 DNAJB1-PRKACA 融合基因的 FL-HCC 患者源性异种移植模型中显示较好的抗肿瘤活性。DS89002333 可用于纤维化肝细胞癌 (FL-HCC) 的研究。

生物活性

DS89002333 is an orally active and potent PRKACA inhibitor, with an IC₅₀ of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC).

体外研究

DS89002333 (0.001, 0.01, 0.1, 1, 10 µM; 30 min) inhibits phosphorylation of CREB in a dose-dependent manner in NIH/3T3 cells (phosphorylation status of CREB as a marker of intracellular PRAKACA inhibitory activity).

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

Cell Viability Assay

Cell Line:	NIH/3T3 cells
Concentration:	0.001, 0.01, 0.1, 1, 10 µM
Incubation Time:	30 min
Result:	Showed a dose-dependent decrease in phosphorylation of CREB, with an IC₅₀ of 50 nM.

体内研究
(In Vivo)

DS89002333 (12.5, 50 mg/kg; p.o.; twice daliy for 5 days) shows anti-tumor activity in an NIH/3T3-fusion allograft model.
DS89002333 (3, 30 mg/kg; p.o.; twice daliy for 22 days) shows significant anti-tumor activity in FL-HCC PDX xenograft model.

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

Animal Model:	Female nude mice (NIH/3T3-fusion allograft model).
Dosage:	12.5, 50 mg/kg
Administration:	Oral administration, twice daliy for 5 days.
Result:	Exhibited anti-tumor activity without body weight loss.

Animal Model:	Female NOD SCID mice (FL-HCC PDX xenograft model).
Dosage:	3, 30 mg/kg
Administration:	Oral administration, twice daliy for 22 days.
Result:	Significant inhibited tumor in mice, and showed temporary body weight loss (at 30 mg/kg), but this resolved following continuous dosing.

体内研究

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

Animal Model:	Female nude mice (NIH/3T3-fusion allograft model).
Dosage:	12.5, 50 mg/kg
Administration:	Oral administration, twice daliy for 5 days.
Result:	Exhibited anti-tumor activity without body weight loss.

Animal Model:	Female NOD SCID mice (FL-HCC PDX xenograft model).
Dosage:	3, 30 mg/kg
Administration:	Oral administration, twice daliy for 22 days.
Result:	Significant inhibited tumor in mice, and showed temporary body weight loss (at 30 mg/kg), but this resolved following continuous dosing.

体内研究

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

Animal Model:	Female nude mice (NIH/3T3-fusion allograft model).
Dosage:	12.5, 50 mg/kg
Administration:	Oral administration, twice daliy for 5 days.
Result:	Exhibited anti-tumor activity without body weight loss.

Animal Model:	Female NOD SCID mice (FL-HCC PDX xenograft model).
Dosage:	3, 30 mg/kg
Administration:	Oral administration, twice daliy for 22 days.
Result:	Significant inhibited tumor in mice, and showed temporary body weight loss (at 30 mg/kg), but this resolved following continuous dosing.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (223.28 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2328 mL	11.1642 mL	22.3284 mL
5 mM	0.4466 mL	2.2328 mL	4.4657 mL
10 mM	0.2233 mL	1.1164 mL	2.2328 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 (sealed storage, away from moisture and light)。-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 (5.58 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.58 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 (5.58 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.58 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 (5.58 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.58 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。