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编 号：F188531
分子式：C26H40Cl4N5O10PS
分子量：787.47
分子式：C26H40Cl4N5O10PS
分子量：787.47
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CAS No: 158382-37-7
产品详情
生物活性：
Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. 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.
体内研究：
Canfosfamide (TER286) exhibits more effective antitumor effect in more frequent administration.Animal Model:BALB/c nude mice (s.c. with tumors of M7609, MX-1 human breast tumor, lung tumor
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.
体外研究：
Canfosfamide (TLK-28) inhibit the catalytic kinase activity of purified DNA-dependent protein kinase (DNA-PK) with an IC50 value of ~1 μM, but causes minimal direct damage to DNA.Canfosfamide (TER286) inhibits MCF-7, NIH-3T3 and M7609 in a dose-dependent manner.
Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. 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.
体内研究：
Canfosfamide (TER286) exhibits more effective antitumor effect in more frequent administration.Animal Model:BALB/c nude mice (s.c. with tumors of M7609, MX-1 human breast tumor, lung tumor
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.
体外研究：
Canfosfamide (TLK-28) inhibit the catalytic kinase activity of purified DNA-dependent protein kinase (DNA-PK) with an IC50 value of ~1 μM, but causes minimal direct damage to DNA.Canfosfamide (TER286) inhibits MCF-7, NIH-3T3 and M7609 in a dose-dependent manner.
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