LomustineAn alkylating antitumor nitrosourea agent

Lomustine (CAS 13010-47-4)

Lomustine | CAS 13010-47-4 is rated 5.0 out of 5 by 1.
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Synonym: 1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea; Belustine; Cecenu; CeeNU; CINU
Application: An alkylating antitumor nitrosourea agent
CAS Number: 13010-47-4
Purity: ≥97%
Molecular Weight: 233.70
Molecular Formula: C9H16CIN3O2
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Lomustine is an alkylating nitrosourea compound that possesses antitumor activity similar to Carmustine (sc-204671) causing DNA interstrand cross-linking. The compound is also a documented inhibitor of glutathione reductase, DLD(lipoamide dehydrogenase) and trypanothione reductase. Lomustine is a highly lipid soluble compound thus enabling it to cross the blood brain barrier and rapidly disperse in tissue. In A2870 cells, Lomustine has been shown to induce p53 expression.


References

1. Dean, S.W., et al. 1986. Biochem. Pharmacol. 35: 1171-1176. PMID: 2938589
2. Hartley, J.A., et al. 1986. Cancer Res. 46: 1943-1947. PMID: 3004713
3. Brent, T.P. 1986. Cancer Res. 46: 2320-2323. PMID: 2938727
4. Aquilina, G., et al. 2000. Clin. Cancer Res. 6: 671-680. PMID: 10690553

Physical State :
Solid
Solubility :
Soluble in ethanol (47 mg/ml at 25° C), chloroform, water (<1 mg/ml at 25° C), DMSO (47 mg/ml at 25° C), and acetone.
Storage :
Store at 4° C
Melting Point :
88-90° C
Boiling Point :
354.07° C (Predicted)
Density :
1.35 g/cm3
Refractive Index :
n20D 1.58
IC50 :
Growth of ZR-75-1: IC50 = 12 µM; Growth of U373: IC50 = 15 µM; HIV-1(RF): IC50 = 42.7 µM (CEM); HIV-1(RF): EC5050 >250 µM (CEM)
pK Values :
pKa: 10.88 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
YS4900000
PubChem CID :
3950
Merck Index :
14: 5564
MDL Number :
MFCD00012392
EC Number :
235-859-2
Beilstein Registry :
2125058
SMILES :
C1CCC(CC1)NC(=O)N(CCCl)N=O

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Certificate of Analysis

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Rated 5 out of 5 by from Harvey Harvey, KA. et al. (PubMed 25526274) reported enhanced anticancer properties of Lomustine when combined with docosahexaenoic acid in glioblastoma cell lines. -SCBT Publication Review
Date published: 2015-05-26
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