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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- CAS No.: 158382-37-7
- Formule: C26H40Cl4N5O10PS
- Masse moléculaire:787.47
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: ~1 µM (DNA-PK)[3]
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Cell Line
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Type | Value | Description | References |
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| B16 | IC50 |
710 nM
Compound: TLK286; Telcyta
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Antiproliferative activity against mouse B16 cells after 72 hrs by MTT assay
Antiproliferative activity against mouse B16 cells after 72 hrs by MTT assay
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[PMID: 29420887] |
| MCF7 | IC50 |
870 nM
Compound: TLK286; Telcyta
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Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
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[PMID: 29420887] |
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[2].
Canfosfamide (TER286) inhibits MCF-7, NIH-3T3 and M7609 in a dose-dependent manner[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, NIH-3T3 and M7609
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Concentration:0-100 μM
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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
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Result:Inhibited these cancer cell lines in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (s.c. with tumors of M7609, MX-1 human breast tumor, lung tumor[3]
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Dosage:150 mg/kg for M7609 xenografts; 400 mg/kg or 200 mg/kg for other xenografts
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Administration:i.v., single dosage for M7609 xenograft; i.p., single dosage for other xenografts; i.p., daily for 5 days
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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.
Chemical Information
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CAS No. 158382-37-7
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Masse moléculaire 787.47
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Formule C26H40Cl4N5O10PS
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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
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Synonyms
TLK-286; TER286
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Canfosfamide Related Classifications
HY-16124 Related Classifications
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