1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis DNA Alkylator/Crosslinker
  3. Cystemustine

Cystemustine is a DNA inhibitor (a chloroethyl nitrosourea, CENU). Cystemustine can cause DNA cross-linking, thereby inhibiting the proliferation of tumor cells. Cystemustine can also exert cytotoxic effects by interfering with the cell cycle, inducing cell re-differentiation, and altering phospholipid metabolism. Cystemustine exhibits high anti-tumor activity and a relatively short plasma half-life in mice. Cystemustine can be used for the study of various malignant tumors, including melanoma, glioma, renal cancer, head and neck cancer, and colorectal cancer, etc.

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

Cystemustine Chemical Structure

Cystemustine Chemical Structure

CAS No. : 79955-36-5

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Description

Cystemustine is a DNA inhibitor (a chloroethyl nitrosourea, CENU). Cystemustine can cause DNA cross-linking, thereby inhibiting the proliferation of tumor cells. Cystemustine can also exert cytotoxic effects by interfering with the cell cycle, inducing cell re-differentiation, and altering phospholipid metabolism. Cystemustine exhibits high anti-tumor activity and a relatively short plasma half-life in mice. Cystemustine can be used for the study of various malignant tumors, including melanoma, glioma, renal cancer, head and neck cancer, and colorectal cancer, etc[1][2][3][4][5][6].

In Vitro

Cystemustine (100, 200 μM, 2 h) causes no significant DNA damage alone, but combination with O6-benzyl-N2-acetylguanosine (BNAG) significantly increases DNA lesions in M3Dau cells[3].
Cystemustine (50 μM, 4 h) causes cytotoxicity causes cytotoxicity in M4Beu cells, but its effect is enhanced when combined with lGgBZ (an O6-alkylguanine-DNA alkyltransferase inhibitor)[6].

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

RT-PCR[3]

Cell Line: M3Dau cells
Concentration: 100, 200 μM or with BNAG (300 μM)
Incubation Time: 2 h or after 4 h
Result: Did not significantly modify the level of amplification of the DNA fragment alone.
Cause 1.85 or 2.55 injuries respectively with combined with BNAG.
In Vivo

Cystemustine (35 mg/kg, i.v., single dose for 55 days) shows a large-amplitude diurnal rhythm toxicity variation with the lowest toxicity level of 15-19 hours after light onset (HALO) and highest level of 7 HALO[2].
Cystemustine (15 mg/kg, i.v. or injected directly into the tumor, at days 1-19) induces deep alterations concerning cell morphology, cell cycle, and melanin content in melanoma mice model[4].
Cystemustine (15 mg/kg, injected directly into the tumor, at days 11-18) makes melanoma tumors a new phospholipid metabolism phenotype in mice model[5].

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

Animal Model: Active span of the rest-activity circadian cycle in male B6DZFI mice (9-10 weeks)[2]
Dosage: 35 mg/kg
Administration: Intravenous injection (i.v.), single dose for 55 days
Result: Survival rate ranged from only 3.8% at HALO up to 87.5 and 88.2% at 15 and 19 HALO, respectively.
Weight loss ranged from -16.6% at 15 HALO to -27.3% at 3 HALO.
Animal Model: Melanoma model established in male C57BL6/6J mice, 6-8 weeks[4]
Dosage: 15 mg/kg
Administration: Intravenous injection (i.v.) or injected directly into the tumor (i.t.), at days 1, 5, and 9 after B16 cell inoculation or at days 11, 14, and 19 after inoculation
Result: Exhibited alteration in cell morphology and increase in melanin content.
Strongly reduced the number of mitoses/microscopic field by 10-fold.
Animal Model: Melanoma model established in male C57BL6/6J mice, 6-8 weeks[5]
Dosage: 15 mg/kg
Administration: Injected directly into the tumor (i.t.), at days 11, 14, and 18 from B16 cell inoculation
Result: Induced a sustained redifferentiation pattern.
Exhibited transient increase in Cho, GPC, and GPE and sustained elevation of PC and PE during growth inhibition.
Exhibited sustained overexpression of PC and PE during growth recovery.
Molecular Weight

257.70

Formula

C6H12ClN3O4S

CAS No.
SMILES

CS(CCNC(N(N=O)CCCl)=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
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    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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Cystemustine
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HY-106435
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