DS89002333
目录号 : GC69015DS89002333 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。
Cas No.:2832159-79-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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)[1].
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)[1].
Cell Viability Assay[1]
| 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. |
DS89002333 (12.5, 50 mg/kg; p.o.; twice daliy for 5 days) shows anti-tumor activity in an NIH/3T3-fusion allograft model[1].
DS89002333 (3, 30 mg/kg; p.o.; twice daliy for 22 days) shows significant anti-tumor activity in FL-HCC PDX xenograft model[1].
| Animal Model: | Female nude mice (NIH/3T3-fusion allograft model)[1]. |
| 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)[1]. |
| 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. |
[1]. Toyota A, et al. ovel protein kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor shows anti-tumor activity in a fibrolamellar hepatocellular carcinoma model. Biochem Biops Res Commun. 2022 Sep 17;621:157-161.
| Cas No. | 2832159-79-0 | SDF | Download SDF |
| 分子式 | C22H20ClF2N3O3 | 分子量 | 447.86 |
| 溶解度 | DMSO : 100 mg/mL (223.28 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture and light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。