Canfosfamide

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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。

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.