1. Apoptosis JAK/STAT Signaling PI3K/Akt/mTOR
  2. Apoptosis Pim mTOR
  3. FD2024

FD2024 是一种泛 PIM 激酶抑制剂,对 PIM-1PIM-2PIM-3IC50 值分别为 0.17 nM、1.86 nM 和 0.38 nM。FD2024 可诱导细胞发生凋亡 (Apoptosis)。FD2024 抑制 mTORp70S6KS64EBP1BAD 蛋白的磷酸化。FD2024 表现出抗急性髓系白血病活性。FD2024 可用于急性髓系白血病的相关研究。

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FD2024

FD2024 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FD2024 is a pan-PIM kinase inhibitor with IC50 values of 0.17 nM, 1.86 nM, and 0.38 nM against PIM-1, PIM-2, and PIM-3, respectively. FD2024 induces cell apoptosis. FD2024 inhibits the phosphorylation of mTOR, p70S6K, S6, 4EBP1, and BAD proteins. FD2024 exhibits anti-acute myeloid leukemia activity. FD2024 can be used in studies related to acute myeloid leukemia[1].

IC50 & Target[1]

PIM1

0.17 nM (IC50)

PIM2

1.86 nM (IC50)

PIM3

0.38 nM (IC50)

体外研究
(In Vitro)

FD2024 可强效抑制 PIM-1、PIM-2 和 PIM-3 激酶,其 IC50 值分别为 0.17 nM、1.86 nM 和 0.38 nM[1]
FD2024 (48 h) 可强效抑制多种人急性髓系白血病 (AML) 细胞系的增殖,其 IC50 值范围为 0.02 μM (MOLM-13) 至 0.25 μM (MOLM-16)[1]
FD2024 (1-5 μM; 48 h) 可剂量依赖性地诱导人急性髓系白血病 (AML) 细胞系发生细胞凋亡,在 MV-4-11 细胞中,5 μM 浓度下的凋亡率显著高于 1 μM 浓度下的凋亡率[1]

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

Apoptosis Analysis[1]

Cell Line: MV-4-11
Concentration: 1 μM, 5 μM
Incubation Time: 48 h
Result: Induced apoptosis in 14.9% of MV-4-11 cells at 1 μM.
Induced apoptosis in 83.8% of MV-4-11 cells at 5 μM.

Western Blot Analysis[1]

Cell Line: EOL-1, MV-4-11
Concentration: 0.1, 0.2, 0.5, 1.0, 2.0, 5.0 μM
Incubation Time: 3 h
Result: Dose-dependently inhibited the phosphorylation of mTOR, p70S6K, S6, 4EBP1, and BAD proteins.
体内研究
(In Vivo)

FD2024 (7.5-15 mg/kg;腹腔注射;每日一次;连续 14 天) 可显著抑制 AML 小鼠模型中的白血病进展,将生存期延长至 44 天,且无全身器官毒性[1]

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

Animal Model: NSFG (NOD-PrkdcscidB6-IL2rgnullNh) (male, 6-8 weeks old, intravenous transplantation of luciferase-expressing MV-4-11 cells)[1]
Dosage: 7.5 mg/kg; 15 mg/kg
Administration: i.p.; daily; 14 days
Result: Suppressed leukemic progression via reduced in vivo bioluminescence intensity.
Prolonged overall survival to 44 days (all vehicle control mice died by day 36).
Showed no treatment-related organ toxicity in liver, heart, spleen, lungs, and kidneys.
Maintained stable body weight throughout the study period.
分子量

440.45

Formula

C22H22F2N6O2

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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FD2024
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HY-181925
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