Pan-RAS-IN-1
目录号 : GC32716
Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins.
Cas No.:1835283-94-7
Sample solution is provided at 25 µL, 10mM.
Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins.
[1] Welsch ME, et al. Multivalent Small-Molecule Pan-RAS Inhibitors. Cell. 2017 Feb 23;168(5):878-889.e29.
Cell experiment: |
For 384-well cancer cell viability assays, cells are trypsinized, counted, and seeded into 384-well plates at 1,000 cells/well. After 16 hr, pan-RAS-IN-1 (from 10 mM stocks in DMSO) are arrayed in an 8-point or 16-point dilution series in 384-well polypropylene plates. Compound solutions are transferred at a 1:5 dilution into the assay plates. After 48 hr, a 50% Alamar blue solution is added to a final concentration of 10% Alamar blue. After 6 hr of incubation, fluorescence intensity is determined at 535 and 590 nm[1]. |
Animal experiment: |
Mice: Mice tumor Xenograft are dosed with 180 mg/kg pan-RAS-IN-1 orally (12 mg/mL, 10% DMSO, pH 4), vehicle orally, or by a combination of i.p. and i.v. injections at 30 mg/kg (4 mg/mL, 5% DMSO in HBSS at pH 4). Over 14 d, mice receive a total of 10 doses of pan-RAS-IN-1 or vehicle orally, or six i.p. injections and 4 i.v. injections. Tumor size is measured by electronic caliper every 2 d and calculated[1]. |
References: [1]. Welsch ME, et al. Multivalent Small-Molecule Pan-RAS Inhibitors. Cell. 2017 Feb 23;168(5):878-889.e29. |
Cas No. | 1835283-94-7 | SDF | |
Canonical SMILES | O=C(C1(N)CCNCC1)NCCCN2C3=CC=C(CN4CCN(CC5=C(Cl)C=CC=C5Cl)CC4)C=C3C(C6=CC=C(OC(F)(F)F)C=C6)=C2 | ||
分子式 | C36H41Cl2F3N6O2 | 分子量 | 717.65 |
溶解度 | DMSO : ≥ 50 mg/mL (69.67 mM) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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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 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 1.3934 mL | 6.9672 mL | 13.9344 mL |
5 mM | 0.2787 mL | 1.3934 mL | 2.7869 mL |
10 mM | 0.1393 mL | 0.6967 mL | 1.3934 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 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet