1. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  2. DNA-PK Apoptosis
  3. 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.

For research use only. We do not sell to patients.

Canfosfamide Chemical Structure

Canfosfamide Chemical Structure

CAS No. : 158382-37-7

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Description

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].

IC50 & Target

IC50: ~1 µM (DNA-PK)[3]

In Vitro

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.

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.
In Vivo

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Molecular Weight

787.47

Formula

C26H40Cl4N5O10PS

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Canfosfamide Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Canfosfamide
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HY-16124
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