LUNA18
目录号 : GC73607LUNA18是一种口服的环肽KRAS和ERK抑制剂。
Cas No.:2676177-63-0
Sample solution is provided at 25 µL, 10mM.
LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer.
LUNA18 (2 μmol/L, 36 h) robustly inhibits proliferation of NCI-H2122, MiaPaCa-2, NCI-H441, LS 180, GSU cell lines, which is a selective RAS inhibitor[3].LUNA18 (0-100 nM, 4 h) decreases GTP-KRAS, pERK1/2 and pAKT expression in a concentration-dependent manner in NCI-H441 cell lines[3].
LUNA18 (10 mg/kg, p.o., once daily for 14 days) results in dose-dependent antitumor activity without any marked body weight loss in NCI-H441 xenograft mouse model[3].PK parameters of LUNA18[3]
References:
[1]. Tanada M, et al. Development of Orally Bioavailable Peptides Targeting an Intracellular Protein: From a Hit to a Clinical KRAS Inhibitor. J Am Chem Soc. 2023 Aug 2;145(30):16610-16620.
[2]. Sase H, et al. Anti-tumor activity of orally-available cyclic peptide LUNA18 through direct RAS inhibition in RAS-altered tumors[J]. Cancer Research, 2024, 84(6_Supplement): 1654-1654. [3]. Ohta A, et al. Validation of a New Methodology to Create Oral Drugs beyond the Rule of 5 for Intracellular Tough Targets[J]. J Am Chem Soc. 2023 Nov 8;145(44):24035-24051.
Cas No. | 2676177-63-0 | SDF | |
分子式 | C73H105F5N12O12 | 分子量 | 1437.68 |
溶解度 | DMSO : ≥ 100 mg/mL (69.56 mM) | 储存条件 | Sealed storage, away from moisture and light, under nitrogen |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 0.6956 mL | 3.4778 mL | 6.9557 mL |
5 mM | 0.1391 mL | 0.6956 mL | 1.3911 mL |
10 mM | 0.0696 mL | 0.3478 mL | 0.6956 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >96.00%
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