2. PI3K/Akt/mTOR
  3. PI4K PI3K
  4. 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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CHMFL-PI4K-127 相关抗体

Top Publications Citing Use of Products

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查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 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.

CHMFL-PI4K-127 相关抗体:
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
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CHMFL-PI4K-127 相关分类

  • 摩尔计算器

  • 稀释计算器

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Keywords:

CHMFL-PI4K-1272377604-81-2PI4KPI3KPhosphatidylinositol 4 kinasesPI4 kinasesPhosphoinositide 3-kinasePI4K kinaseKinase inhibitorMalariaBlood stageLiver stageantimalariaInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-150598
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