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Canfosfamide
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。
Canfosfamide图片
CAS NO:158382-37-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
TLK-286
TER286
产品介绍
Canfosfamide (TLK-286) 是一种谷胱甘肽类似物前体药物,由谷胱甘肽 S-转移酶 P1-1 激活,诱导细胞凋亡 (apoptosis)。Canfosfamide还抑制 DNA 依赖性蛋白激酶 (DNA-PK) 的催化激酶活性。Canfosfamide 在活化后产生一种抗癌烷基化剂和谷胱甘肽衍生物。Canfosfamide 可用于恶性肿瘤的研究。
生物活性

Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and inducesapoptosis. Canfosfamide also inhibits the catalytic kinase activity of DNA-dependent protein kinase (DNA-PK). Canfosfamide produces an anticancer alkylating agent and a glutathione derivative after activation. Canfosfamide can be used to research malignancies[1][2][3].

IC50& Target

IC50: ~1 μM (DNA-PK)[3]

体外研究
(In Vitro)

Canfosfamide (TLK-28) inhibit the catalytic kinase activity of purified DNA-dependent protein kinase (DNA-PK) with an IC50value of ~1 μM, but causes minimal direct damage to DNA[2].
Canfosfamide (TER286) inhibits MCF-7, NIH-3T3 and M7609 in a dose-dependent manner[3].

Cell Proliferation Assay[3]

Cell Line:MCF-7, NIH-3T3 and M7609
Concentration:0-100 μM
Incubation Time:Co-incubated for 2 h then removed and incubated for 5 days in MCF-7; co-incubated for 10 days in NIH-3T3; co-incubated for 48 h in M7609
Result:Inhibited these cancer cell lines in a dose-dependent manner.
体内研究
(In Vivo)

Canfosfamide (TER286) exhibits more effective antitumor effect in more frequent administration[3].

Animal Model:BALB/c nude mice (s.c. with tumors of M7609, MX-1 human breast tumor, lung tumor[3]
Dosage:150 mg/kg for M7609 xenografts; 400 mg/kg or 200 mg/kg for other xenografts
Administration:i.v., single dosage for M7609 xenograft; i.p., single dosage for other xenografts; i.p., daily for 5 days
Result:The best response to TER286 was for the MX-1 human breast tumor treated with an aggressive regimen (daily for 5 days), under which nearly all of the tumors were either severely growth inhibited or substantially regressed.
Clinical Trial
分子量

787.47

Formula

C26H40Cl4N5O10PS

CAS 号

158382-37-7

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.