Lomeguatrib
- Product Name
- Lomeguatrib
- CAS No.
- 192441-08-0
- Chemical Name
- Lomeguatrib
- Synonyms
- C521206;CS-1103;AI3 27596;BRN1861032;Lomeguatrib;Lomeguqtrib;BRN 1861032;BRN-1861032;Lomeguaritrib;Lomeguatrib, >=98%
- CBNumber
- CB11261272
- Molecular Formula
- C10H8BrN5OS
- Formula Weight
- 326.17
- MOL File
- 192441-08-0.mol
Lomeguatrib Property
- Boiling point:
- 683.8±65.0 °C(Predicted)
- Density
- 2.07
- storage temp.
- Keep in dark place,Inert atmosphere,2-8°C
- solubility
- DMSO: soluble10mg/mL, clear
- pka
- 9.42±0.10(Predicted)
- form
- powder
- color
- white to beige
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML0586
- Product name
- Lomeguatrib
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $128
- Updated
- 2024/03/01
- Product number
- SML0586
- Product name
- Lomeguatrib
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $397
- Updated
- 2024/03/01
- Product number
- 11732
- Product name
- Lomeguatrib
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $38
- Updated
- 2024/03/01
- Product number
- 11732
- Product name
- Lomeguatrib
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $67
- Updated
- 2024/03/01
- Product number
- 11732
- Product name
- Lomeguatrib
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $146
- Updated
- 2024/03/01
Lomeguatrib Chemical Properties,Usage,Production
Description
Lomeguatrib (192441-08-0) is a potent (IC50?= 9 nM) inhibitor of O6-Methylguanine-DNA Methyltransferase (MGMT), an important DNA repair protein.1?It is currently being investigated in cancers that have acquired resistant to the chemotherapeutic temozolomide2-5, as well as other chemotherapeutics6,7.
Uses
O6-Methylguanine-DNA methyltransferase (MGMT) is a DNA repair protein which removes an alkyl group from the O6 position on guanine in an autoinactivating reaction. Although important in normal DNA repair, this reaction confers resistance to treatments that use O6-alkylating agents to produce cytotoxicity, e.g., in cancer. Lomeguatrib is a modified quanine base which acts as a pseudosubstrate inactivator of MGMT (IC50 = ~3 nM). A non-toxic compound, lomeguatrib completely inactivates MGMT in human prostate and colorectal tumors when given as a single 120 mg oral dose and in primary central nervous system cancers at 160 mg.
Uses
Lomeguatrib is an inhibitor of O6-methylguanine-DNA methyltransferase (MGMT). Lomeguatrib attenuates MGMT activity in vitro and in vivo. Lomeguatrib enhances the antitumor activity of temozolomide in both human melanoma and MCF-7 xenografts.
storage
+4°C
References
1) Reinhard?et al.?(2001),?Monosaccharide-Linked Inhibitors of O6-Methylguanine-DNA Methyltransferase (MGMT): Synthesis, Molecular Modeling, and Structure-Activity Relationships; J. Med. Chem.?44?4050 2) Barvaux?et al.?(2004),?Sensitization of a human ovarian cancer cell line to temozolomide by simultaneous attenuation of the Bcl-2 antiapoptotic protein and DNA repair by O6-alkylguanine-DNA alkyltransferase: Mol. Cancer Ther.?3?1215 3) Gumbrell?et al.?(2006),?Lomeguatrib, a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase: phase I safety, pharmacodynamic, and pharmacokinetic trial and evaluation in combination with temozolomide in patients with advanced solid tumors: Clin. Cancer Res.?12?1577 4) Watson?et al.?(2009),?O(6)-methylguanine-DNA methyltransferase depletion and DNA damage in patients with melanoma treated with temozolomide alone or with lomeguatrib: Br. J. Cancer?100?1250 5) Taspinar?et al.?(2013),?Effect of lomeguatrib-temozolomide combination of MGMT promoter methylation and expression in primary glioblastoma tumor cells: Tumour Biol.?34?1935 6) Sabharwal?et al.?(2010),?A phase I trial of lomeguatrib and irinotecan in metastatic colorectal cancer: Cancer Chemother. Pharmacol.?66?829 7) Tawbi?et al.?(2011),?Inhibition of DNA repair with MGMT pseudosubstrates: phase I study of lomeguatrib in combination with dacarbazine in patients with advanced melanoma and other solid tumors: Br. J. Cancer?105?773
Lomeguatrib Preparation Products And Raw materials
Raw materials
Preparation Products
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