1. PI3K/Akt/mTOR
  2. PI4K PI3K
  3. CHMFL-PI4K-127

CHMFL-PI4K-127 (compound 15g) 是一种口服有效、高选择性的 PfPI4K (恶性疟原虫 PI4K 激酶)抑制剂,IC50 为 0.9 nM。CHMFL-PI4K-127 对 3D7 恶性疟原虫表现出较强的抑制活性,其 EC50 为 25.1 nM。CHMFL-PI4K-127 显示了抗疟疾作用。

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CHMFL-PI4K-127 Chemical Structure

CHMFL-PI4K-127 Chemical Structure

CAS No. : 2377604-81-2

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10 mg ¥1920
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25 mg ¥3840
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy[1].

IC50 & Target

PI4K

0.9 ± 0.1 nM (IC50)

PI3Kδ

104 ± 3 nM (IC50)

PI3Kα

191 ± 36 nM (IC50)

PI3Kγ

324 ± 19 nM (IC50)

PI3Kβ

392 ± 27 nM (IC50)

Vps34

681 ± 25 nM (IC50)

体外研究
(In Vitro)

CHMFL-PI4K-127 (compound 15g) displays high selectivity against PfPI4K over human lipid and protein kinase[1].
CHMFL-PI4K-127 exhibits EC50 values of 23–47 nM against a panel of the drug-resistant strains of P. falciparum[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

CHMFL-PI4K-127 (compound 15g) (Orally; 0-80 mg/kg/day for 7 days; 0-15 mg/kg, once) exhibits the antimalaria efficacy in both blood stage (80 mg/kg) and liver stage (1 mg/kg) of Plasmodium in infected rodent model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c mice were infected by P. yoelii[1].
Dosage: 0, 60, 80 mg/kg
Administration: Orally, daily for 7 days
Result: Displayed significant in vivo antimalarial activities in a dose-dependent manner and 80 mg/kg × 7 days treatment generated curative effects. The 60 mg/kg dosage resulted in suppressive effects during the drug treatment but relapsed after stopping treatment.
Animal Model: Balb/c mice were infected by P. yoelii[1].
Dosage: 0, 1, 5, 15 mg/kg
Administration: Orally, once
Result: Provided the full protection and cure at 1 mg/kg with no negligible parasite visible in the liver of all tested mice at 24, 48, 72, 96, 144 and 196 h, indicating true causal prophylactic efficacy.
分子量

402.85

Formula

C18H15ClN4O3S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (310.29 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4823 mL 12.4116 mL 24.8231 mL
5 mM 0.4965 mL 2.4823 mL 4.9646 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

CHMFL-PI4K-127 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4823 mL 12.4116 mL 24.8231 mL 62.0578 mL
5 mM 0.4965 mL 2.4823 mL 4.9646 mL 12.4116 mL
10 mM 0.2482 mL 1.2412 mL 2.4823 mL 6.2058 mL
15 mM 0.1655 mL 0.8274 mL 1.6549 mL 4.1372 mL
20 mM 0.1241 mL 0.6206 mL 1.2412 mL 3.1029 mL
25 mM 0.0993 mL 0.4965 mL 0.9929 mL 2.4823 mL
30 mM 0.0827 mL 0.4137 mL 0.8274 mL 2.0686 mL
40 mM 0.0621 mL 0.3103 mL 0.6206 mL 1.5514 mL
50 mM 0.0496 mL 0.2482 mL 0.4965 mL 1.2412 mL
60 mM 0.0414 mL 0.2069 mL 0.4137 mL 1.0343 mL
80 mM 0.0310 mL 0.1551 mL 0.3103 mL 0.7757 mL
100 mM 0.0248 mL 0.1241 mL 0.2482 mL 0.6206 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CHMFL-PI4K-127
目录号:
HY-150598
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