KDU691
目录号 : GC32118
An antimalarial compound
Cas No.:1513879-19-0
Sample solution is provided at 25 µL, 10mM.
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KDU691 is an antimalarial compound.1 It inhibits recombinant P. vivax phosphatidylinositol 4-kinase (PI4K) with an IC50 value of 1.5 nM. KDU691 is selective for P. vivax PI4K over recombinant human PI4KβIII and PI3Kα, -β, -?, and -δ (IC50s = 7.9, 8.8, 2.4, 8, and 3.4 ?M, respectively), as well as VPS34 (IC50 = >9.7 ?M) and 36 additional kinases in a panel of lipid and protein kinases (IC50s = >10 ?M). It is active against P. falciparum and P. yoelii schizonts (IC50s = 0.06 and 0.04 ?M, respectively), as well as P. cynomolgi schizonts and hypnozoites (IC50s = 0.11 and 0.2 ?M, respectively).2 KDU691 completely prevents, but does not eradicate established, P. cynomolgi infection in rhesus monkeys when administered at a dose of 20 mg/kg.3
1.McNamara, C.W., Lee, M.C., Lim, C.S., et al.Targeting Plasmodium phosphatidylinositol 4-kinase to eliminate malariaNature504(7479)248-253(2013) 2.Zou, B., Nagle, A., Chatterjee, A.K., et al.Lead optimization of imidazopyrazines: a new class of antimalarial with activity on Plasmodium liver stagesACS Med. Chem. Lett.5(8)947-950(2014) 3.Zeeman, A.M., Lakshminarayana, S.B., van der Werff, N., et al.PI4 kinase is a prophylactic but not radical curative target in Plasmodium vivax-type malaria parasitesAntimicrob. Agents Chemother.60(5)2858-2863(2016)
Animal experiment: | For in vivo PK studies, female CD-1 mice (25 to 30g) are used and randomly assigned to cages. Mice are allowed to acclimate before initiation of the experiments. Feed and water are given ad libitum. KDU691 is formulated at concentrations of 2.5 mg/mL and 0.25 mg/mL for a dose of 25 mg/kg and 2.5 mg/kg, respectively. The suspension formulation for p.o. dosing contains 0.5% Methyl cellulose and 0.5% Tween 80 in water. After oral dosing, blood and liver samples from mice are collected at 0.08 to 24 h post dosing. Groups of three mice are used for each time point. Blood is centrifuged at 13,000 rpm for 7 min at 4°C, plasma harvested and stored at -20°C until analysis. Liver tissue samples are excised, dipped in PBS, gently blotted with absorbent paper, dried, weighed and stored at -20°C until further analysis[1]. |
References: [1]. Zeeman AM, et al. PI4 Kinase Is a Prophylactic but Not Radical Curative Target in Plasmodium vivax-Type Malaria Parasites. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2858-63. | |
| Cas No. | 1513879-19-0 | SDF | |
| Canonical SMILES | ClC1=CC=C(N(C(C2=CN3C(C=N2)=NC=C3C4=CC=C(C(NC)=O)C=C4)=O)C)C=C1 | ||
| 分子式 | C22H18ClN5O2 | 分子量 | 419.86 |
| 溶解度 | DMSO : 150 mg/mL (357.26 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 | 2.3817 mL | 11.9087 mL | 23.8175 mL |
| 5 mM | 0.4763 mL | 2.3817 mL | 4.7635 mL |
| 10 mM | 0.2382 mL | 1.1909 mL | 2.3817 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet