158382-37-7
Chemical Structure
Canfosfamide
Synonym(s): TLK-286; TER286
- CAS No.: 158382-37-7
- Formula:C26H40Cl4N5O10PS
- Molecular Weight:787.47
IUPAC Name: N5-((R)-3-((2-((bis(bis(2-chloroethyl)amino)phosphoryl)oxy)ethyl)sulfonyl)-1-(((R)-carboxy(phenyl)methyl)amino)-1-oxopropan-2-yl)-L-glutamine
InChIKey: OJLHWPALWODJPQ-QNWVGRARSA-N
SMILES: ClCCN(CCCl)P(N(CCCl)CCCl)(OCCS(C[C@H](NC(CC[C@H](N)C(O)=O)=O)C(N[C@H](C1=CC=CC=C1)C(O)=O)=O)(=O)=O)=O
Biological Activity: 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[1][2][3].
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Canfosfamide | 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. | |||||||||||||||||||||
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References
- [1]. Dourado DF, et al. Mechanism of glutathione transferase P1-1-catalyzed activation of the prodrug canfosfamide (TLK286, TELCYTA). Biochemistry. 2013 Nov 12;52(45):8069-78. [Content Brief]
- [2]. Tew KD. TLK-286: a novel glutathione S-transferase-activated prodrug. Expert Opin Investig Drugs. 2005 Aug;14(8):1047-54. [Content Brief]
- [3]. Morgan AS, et al. Tumor efficacy and bone marrow-sparing properties of TER286, a cytotoxin activated by glutathione S-transferase. Cancer Res. 1998 Jun 15;58(12):2568-75. [Content Brief]
