PTC-209 hydrobromide

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CAS NO:

1217022-63-3

PTC-209 hydrobromide 是一种特定的BMI-1抑制剂，在 HEK293T 细胞系中的IC₅₀为 0.5 μM。PTC-209 hydrobromide 不可逆转地损害结直肠癌起始细胞 (CICs)。PTC-209 hydrobromide 显示有效的抗骨髓瘤活性并损害肿瘤微环境。

生物活性

PTC-209 hydrobromide is a specificBMI-1inhibitor with anIC₅₀of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment^[1]^[2].

IC₅₀& Target

IC50: 0.5 μM (BMI-1, in HT1080 tumor cells)^[1]

体外研究
(In Vitro)

PTC-209 (0.01-10 μM; 24-72 hours) induces a concentration- and time-dependent decrease in the cellular viability of all cell lines tested^[2].
PTC-209 (1-2.5 μM) inhibits STAT3 phosphorylation in A549 lung cancer cells and MDA-MB-231 breast cancer cells^[2].

Cell Viability Assay^[2]

Cell Line:	Lung (LNM35, A549 cells), breast (MDA-MB-231 and T47D cells), and colon (HT-29, HCT-116, and HCT8/S11 cells)
Concentration:	0.01-10 μM
Incubation Time:	24, 48, and 72 hour
Result:	Induced a concentration- and time-dependent decrease in the cellular viability of all cell lines tested.

体内研究
(In Vivo)

PTC-209 (60 mg/kg body weight; subcutaneously; once a day for 11 days) significantly reduces tumor volume^[2].

Animal Model:	Nude mice (male, aged 8-10 weeks, HCT1116 cell-derived tumor)^[1]
Dosage:	60 mg/kg body weight
Administration:	Subcutaneously; once a day for 11 days
Result:	Significantly reduced tumor volume.

分子量

576.10

Formula

C₁₇H₁₄Br₃N₅OS

CAS 号

1217022-63-3

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.