DS89002333

立即咨询

DS89002333

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2832159-79-0

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 potentPRKACAinhibitor, with anIC₅₀of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing theDNAJB1-PRKACAfusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC)^[1].

IC₅₀& Target

PRKACA

0.3 nM (IC₅₀)

体外研究
(In Vitro)

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 IC₅₀of 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^[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.

分子量

447.86

Formula

C₂₂H₂₀ClF₂N₃O₃

CAS 号

2832159-79-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.