STF-118804
(Synonyms: 烟酰胺磷酸核糖基转移酶) 目录号 : GC17096
A Nampt inhibitor
Cas No.:894187-61-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
STF-118804 is an inhibitor of NAMPT [1].
Nicotinamide phosphoribosyl transferase (NAMPT) is a rate-limiting enzyme in the biosynthesis of nicotinamide adenine dinucleotide (NAD+), an important cofactor in many biochemical and biological processes. Also, NAMPT is a cytokine that inhibits neutrophil apoptosis and promotes B cell maturation [1].
STF-118804 is a NAMPT inhibitor. In B-ALL cell lines, STF-118804 reduced the viability with high potency. In leukemic samples from pediatric acute lymphoblastic leukemia (ALL) patients, STF-118804 reduced the viability with IC50 values of 3.1-32.3 nM. In MV411 cells, STF-118804 induced apoptosis without cell cycle arrest. Also, STF-118804 showed high potency in colon and prostate cell lines. STF-118804 (10 μM) inhibited NAD+ production from nicotinamide. In 293T cells over-expressing NAMPT, STF-118804 reduced the viability with IC50 value of 106 nM. However, STF-118804 had no effect on cells over-expressing H191R or G217R mutants [1].
In mice bearing orthotopic xenograft model of ALL, STF-118804 increased survival and inhibited tumor growth. Also, STF-118804 effectively reduced leukemia stem cells [1].
Reference:
[1]. Matheny CJ, Wei MC, Bassik MC, et al. Next-generation NAMPT inhibitors identified by sequential high-throughput phenotypic chemical and functional genomic screens. Chem Biol, 2013, 20(11): 1352-1363.
| Cas No. | 894187-61-2 | SDF | |
| 别名 | 烟酰胺磷酸核糖基转移酶 | ||
| 化学名 | 4-[5-methyl-4-[(4-methylphenyl)sulfonylmethyl]-1,3-oxazol-2-yl]-N-(pyridin-3-ylmethyl)benzamide | ||
| Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)CC2=C(OC(=N2)C3=CC=C(C=C3)C(=O)NCC4=CN=CC=C4)C | ||
| 分子式 | C25H23N3O4S | 分子量 | 461.53 |
| 溶解度 | ≥ 19.1mg/mL in DMSO | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1667 mL | 10.8335 mL | 21.6671 mL |
| 5 mM | 0.4333 mL | 2.1667 mL | 4.3334 mL |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1667 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。