2. Cell Cycle/DNA Damage
  3. Eukaryotic Initiation Factor (eIF)
  4. APL-4098

APL-4098 是一种具有口服活性的、选择性的、 ATP 竞争性的 GCN2 抑制剂，其 Ki 为 4.39 nM，Kd 为 2.9 nM。APL-4098 可降低 eIF2α 的磷酸化水平及 ATF4 的表达量。APL-4098 损伤线粒体功能，对原代急性髓系白血病细胞具有细胞毒性作用。APL-4098 可用于急性髓系白血病的相关研究。

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APL-4098

APL-4098 Chemical Structure

CAS No. : 2752441-61-3

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APL-4098 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

APL-4098 is an orally active, selective, ATP-competitive GCN2 inhibitor with a Ki of 4.39 nM and a Kd of 2.9 nM. APL-4098 reduces the phosphorylation level of eIF2α and the expression level of ATF4. APL-4098 impairs mitochondrial function and exerts cytotoxic effects on primary acute myeloid leukemia cells. APL-4098 is applicable to research related to acute myeloid leukemia[1].

IC50 & Target[1]

eIF2

 

体外研究
(In Vitro)

APL-4098 (0-1 μM; 4 h) 呈剂量依赖性降低谷氨酰胺缺乏的 U2OS 骨肉瘤细胞中 eIF2α 的磷酸化水平及 ATF4 蛋白的表达[1]。
APL-4098 (0.1-1 μM) 可在体外诱导患者原代 AML 细胞发生细胞死亡，在部分样本中还对富集白血病干细胞 (LSC) 的 CD34+/CD38-亚群产生细胞毒性作用[1]。
APL-4098 (250 nM; 6-24 h) 可降低 MOLM-16 急性髓系白血病 (AML) 细胞的线粒体膜电位[1]。
APL-4098 (0-1 μM; 24 h) 可呈剂量依赖性抑制 MOLM-16 急性髓系白血病 (AML) 细胞的线粒体呼吸[1]。

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

APL-4098 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CL Vd T1/2 Bioavailability
Rat[1] 1 mg/kg i.v. 0.08 mL/min/kg 0.11 L/kg 18.1 h /
Rat[1] 3 mg/kg p.o. / / / 66 %
体内研究
(In Vivo)

APL-4098 (0.5-5 mg/kg；口服；每日 1 次；连续 11 天) 可在皮下 AML CDX 模型中诱导剂量依赖性的肿瘤生长抑制[1]。
APL-4098 (15 mg/kg；口服；每日 1 次；连续 19 天) 可在患者来源的 AML PDX 模型中选择性清除富含 LSC 的 CD34+/CD38−亚群，而对整体白血病负荷的影响极小[1]。

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

Animal Model: NOD/SCID (female, 6-8 weeks old, subcutaneous AML CDX model)[1]
Dosage: 0.5 mg/kg; 1.5 mg/kg; 5 mg/kg
Administration: p.o.; once daily; 11 days
Result: Achieved 46.2% TGI at 0.5 mg/kg with low unbound plasma exposure.
Showed intermediate TGI at 1.5 mg/kg with increased unbound plasma exposure.
Reached 98.3% TGI at 5 mg/kg with the highest unbound plasma exposure.
Caused no notable consistent adverse events, including no relevant effect on body weight or survival.
Animal Model: NOG (female, 6-8 weeks old, patient-derived AML PDX model)[1]
Dosage: 15 mg/kg
Administration: p.o.; once daily; 19 days
Result: Exerted minimal effect on bulk leukemia (percentage of viable hCD45+ cells).
Pronounced and selectively depleted the LSC-enriched CD34+/CD38- subpopulation, significantly reducing cell numbers relative to vehicle control.
Caused no apparent cytotoxicity in experimental animals.
分子量

434.83

Formula

C17H12ClFN6O3S
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

APL-4098 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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.

Keywords:

APL-40982752441-61-3APL4098APL 4098Eukaryotic Initiation Factor (eIF)patient-derived xenograft modelsmitochondrial functionCD34+/CD38- subpopulationMOLM-16 AML cellsGCN2cell line-derived xenograft modelsacute myeloid leukemia cellseIF2αATF4mitochondrial oxidative phosphorylationInhibitorinhibitorinhibit

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产品名称：
APL-4098
目录号：
HY-181959
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