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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。
DS89002333图片
CAS NO:2832159-79-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

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 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.