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

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.

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FD2024

FD2024 Chemical Structure

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Description

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)

In Vitro

FD2024 potently inhibits PIM-1, PIM-2, and PIM-3 kinases with IC50 values of 0.17 nM, 1.86 nM, and 0.38 nM, respectively[1].
FD2024 (48 h) potently inhibits the proliferation of multiple human AML cell lines, with IC50 values ranging from 0.02 μM (MOLM-13) to 0.25 μM (MOLM-16)[1].
FD2024 (1-5 μM; 48 h) dose-dependently induces apoptosis in human AML cell lines, with significantly higher apoptotic rates at 5 μM compared to 1 μM in both MV-4-11 and EOL-1 cells[1].

MedChemExpress (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.
In Vivo

FD2024 (7.5-15 mg/kg; i.p.; daily; 14 days) significantly suppresses leukemic progression in an AML mouse model, prolongs survival to 44 days, and shows no systemic organ toxicity[1].

MedChemExpress (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.
Molecular Weight

440.45

Formula

C22H22F2N6O2

SMILES

FC(C=CC=C1F)=C1C2=NC(C(NC3=C(O[C@@H]4CC[C@@H](N)CC4)C=CN=C3)=O)=C(N)N=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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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
Cat. No.:
HY-181925
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