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/ Lomustine/洛莫司汀

Lomustine/洛莫司汀 {[allProObj[0].p_purity_real_show]}

货号：A447678 同义名： CCNU; NSC 79037

Lomustine is an alkylating nitrosourea compound used in chemotherapy. Lomustine (420 μM) triggers apoptosis through the mitochondrial pathway via decrease in the level of the anti-apoptosis proteins Bcl-2 and Bcl-xl, respectively, in both medulloblastoma and normal human epithelial and fibroblast cells. Lomustine induces cell cycle delay in G2/M phase in medulloblastoma cells and up-regulates p21 protein level in a p53-independent manner in HFSN1 cells.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Lomustine/洛莫司汀 化学结构 CAS号：13010-47-4
Lomustine/洛莫司汀 化学结构
CAS号：13010-47-4
Lomustine/洛莫司汀 3D分子结构
CAS号：13010-47-4
Lomustine/洛莫司汀 化学结构 CAS号：13010-47-4
Lomustine/洛莫司汀 3D分子结构 CAS号：13010-47-4
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Lomustine/洛莫司汀 纯度/质量文件 产品仅供科研

货号：A447678 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 DNA synthesis ↓ helicase ↓ RdRp ↓ ribonucleotide reductase ↓ tRNA synthetase ↓ YB-1 ↓ 其他靶点 纯度
Fexinidazole ✔ 98%
Daptomycin ✔ 98%
Blasticidin S·HCl ✔ 98%
Metronidazole ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Triglycidyl isocyanurate ✔ p53 98+%
Nedaplatin ✔ 99%+
Oxolinic acid ✔ 98+%
Bendamustine ✔ 98+%
Trifluridine ✔ 98%
Robinetin ✔ 99%+
Carboplatin ✔ 99%
Cidofovir ✔ 99%
Cisplatin ✔ 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

 		98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

 		99%+
Oxaliplatin ✔ 98%
YK-4-279 ✔ 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

 		99%+
RK-33 ✔ 98%
Brr2-IN-3 ✔ 99%+
Phen-DC3 Trifluoromethanesulfonate ✔ 95%
Favipiravir ✔ 99%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

 		99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

 		97%
Didox ✔ 98%
(E)-3-AP ✔ 99%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

 		99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, IC50: 46.11 nM

Leucyl-tRNA synthetase, Kd: 42.1 nM

 		98%
SU056 +

YB-1, IC50: 1.73 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Lomustine/洛莫司汀 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]

Lomustine/洛莫司汀 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 <<

Lomustine/洛莫司汀 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

Lomustine/洛莫司汀 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.28mL

0.86mL

0.43mL

21.39mL

4.28mL

2.14mL

42.79mL

8.56mL

4.28mL

Lomustine/洛莫司汀 技术信息

CAS号13010-47-4
分子式C9H16ClN3O2
分子量 233.7
SMILES Code O=C(NC1CCCCC1)N(CCCl)N=O
MDL No. MFCD00012392
别名 CCNU; NSC 79037; WR139017.; Prava. CCNU. Acronym: CCNU. RB1509; Lucostine; Lucostin; Lomeblastin; Citostal; Cecenu; Belustine; Belustin; Lomustinume. CeeNU; NCI C04740; CeeNU; Gleostine
运输蓝冰
InChI Key GQYIWUVLTXOXAJ-UHFFFAOYSA-N
Pubchem ID 3950
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, store in freezer, under -20°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: Lomustine | 13010-47-4 | CCNU | NSC 79037 | NSC79037 | NSC 79037 | NSC-79037 | Cell Cycle/DNA Damage | Autophagy | Apoptosis | DNA Alkylator/Crosslinker | Autophagy | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lomustine/洛莫司汀 纯度/质量文件 | Lomustine/洛莫司汀 亚型比较 | Lomustine/洛莫司汀 生物活性 | Lomustine/洛莫司汀 临床数据 | Lomustine/洛莫司汀 参考文献 | Lomustine/洛莫司汀 实验方案 | Lomustine/洛莫司汀 技术信息

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