Lomustine

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Chemical Structure| 13010-47-4 同义名 : CCNU;NSC 79037;WR139017.;Prava. CCNU. Acronym: CCNU. RB1509;Lucostine;Lucostin;Lomeblastin;Citostal;Cecenu;Belustine;Belustin;Lomustinume. CeeNU;NCI C04740;CeeNU;Gleostine
CAS号 : 13010-47-4
货号 : A447678
分子式 : C9H16ClN3O2
纯度 : 99%+
分子量 : 233.695
MDL号 : MFCD00012392
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(449.3 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Lomustine is a DNA alkylating agent, with antitumor activity. Lomustine is cytotoxic to the U87-MG cells expressing tumor-derived mutant IDH1, and has little effect on the expression of wild-type IDH1. Administered lomustine 20mg/kg in mice,the absorption was extremely rapid, with peak plasma concentration being reached within 2 min after injection. [4]. Lomustine suppresses U87-MG growth with an ED50 of 68.1 μM. Lomustine(30, 40 μM) in combination with docosahexaenoic acid (DHA), the combination also resulted in growth inhibition of 2 additional human-derived glioblastoma cell lines, DB029 and MHBT161.[5]. Lomustine(30 mg/kg) in combination with Toca 511 + 5-FC prolongs survival in rats bearing F98 tumor cells, and also exhibits antitumor activity in the B6C3F1 mice bearing Tu-2449 glioma cells. [6]. Lomustine for treatment of mast cell tumors in 38 cats, targeted lomustine dosage was 50 mg/m2 in 22 cats and 60 mg/m2 in 16 cats. Median administered dosage of lomustine was 56 mg/m2 (range, 48 to 65 mg/m2).[7].
作用机制 Lomustine is a monofunctional alkylating agent, it alkylates DNA and RNA , it can also cross-link DNA and thus acts in a cell cycle-dependent and -independent manner. [3]
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02551718 Acute Leukemia of Ambiguous Li... 展开 >>neage Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Acute Myeloid Leukemia Recurrent Childhood Acute Lymphoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Refractory Acute Myeloid Leukemia Refractory Adult Acute Lymphoblastic Leukemia Refractory Childhood Acute Lymphoblastic Leukemia 收起 << Not Applicable Recruiting - United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Pamela S. Becker    206-616-1589    pbecker@u.washington.edu    Principal Investigator: Pamela S. Becker 收起 <<
NCT00303810 Brain and Central Nervous Syst... 展开 >>em Tumors 收起 << Not Applicable Completed - Germany ... 展开 >> University Medical Center Hamburg - Eppendorf Hamburg, Germany, D-20246 收起 <<
NCT00278278 Brain and Central Nervous Syst... 展开 >>em Tumors 收起 << Phase 3 Unknown - United States, Texas ... 展开 >> M. D. Anderson Cancer Center at University of Texas Houston, Texas, United States, 77030-4009 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.28mL

0.86mL

0.43mL

21.40mL

4.28mL

2.14mL

42.79mL

8.56mL

4.28mL
参考文献

[1]Shinwari Z, Manogaran PS, et al.Vincristine and lomustine induce apoptosis and p21(WAF1) up-regulation in medulloblastoma and normal human epithelial and fibroblast cells. J Neurooncol. 2008 Apr;87(2):123-32.

[2]Rassnick KM, Moore AS, et al. Treatment of canine mast cell tumors with CCNU (lomustine). J Vet Intern Med. 1999 Nov-Dec;13(6):601-5.

[3] Michael Weller ,et al. How did lomustine become standard of care in recurrent glioblastoma? Cancer Treatment Reviews 87 (2020) 102029.

[4] F Y Lee, P Workman, Modification of CCNU pharmacokinetics by misonidazole--a major mechanism of chemosensitization in mice, Br J Cancer. 1983 May;47(5):659-69.

[5] Harvey KA, et al. Enhanced anticancer properties of lomustine in conjunction with docosahexaenoic acid in glioblastoma cell lines. J Neurosurg. 2015 Mar;122(3):547-56.

[6]Yagiz K, et al. Toca 511 plus 5-fluorocytosine in combination with lom-ustine shows chemotoxic and immunotherapeutic activity with no additive toxicity in rodent glioblastoma models. Neuro Oncol. 2016 Oct;18(10):1390-401.

[7] Kenneth M,et al. Lomustine for treatment of mast cell tumors in cats: 38 cases (1999–2005), J Am Vet Med Assoc. 2008 Apr 15;232(8):1200-5