1. Protein Tyrosine Kinase/RTK
    Epigenetics
    Cell Cycle/DNA Damage
  2. FLT3
    HDAC
  3. Crotonoside

Crotonoside (Synonyms: Isoguanosine)

Cat. No.: HY-N0071
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Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the treatment of AML.

For research use only. We do not sell to patients.

Crotonoside Chemical Structure

Crotonoside Chemical Structure

CAS No. : 1818-71-9

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Description

Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the treatment of AML[1].

IC50 & Target[1]

FLT3

 

HDAC3

 

HDAC6

 

In Vitro

Crotonoside (0-200 μM;) selectively inhibits the viability of AML cell line MV4-11, MOLM-13 (with FLT3-ITD mutant) and KG-1 (without FLT3-ITD mutant) in a dose-dependent manner with an IC50 of 11.6 μM, 12.7 μM and 17.2 μM, respectively[1].
Crotonoside (0-100μM; 7 hours) inhibits the phosphorylation of FLT3 Erk1/2, Akt/mTOR and STAT5 is strongly inhibited by crotonoside at higher concentration of 12.5 μM in a concentration-dependent manner[1].
Crotonoside (0-100 μM; 12 hours) exhibits a dose-dependent increase in the percentage of G0/G1 phase and a dose-dependent decrease in the percentage of G2/M and S phases cells[1].
Crotonoside (0-100 μM; 24 hours) leads to concentration-dependent changes in the number of apoptotic MV4-11 cells, results in a dose-dependent decrease in the level of pro-caspase-3 and a dose-dependent increase in the level of the cleaved caspase-3 fragments[1].

Cell Viability Assay[1]

Cell Line: AML cell line MV4-11, MOLM-13 and KG-1 cells
Concentration: 0-200 μM
Incubation Time: 72 hours
Result: Inhibited AML cells growth than other cell lines tested.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM
Incubation Time: 7 hours
Result: Inhibited AML cells growth than other cell lines tested.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM
Incubation Time: 12 hours
Result: Induced cell cycle arrest in G0/G1.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM
Incubation Time: 24 hours
Result: Induced MV4-11 cell apoptosis.
In Vivo

Crotonoside(intraperitoneal and intravenous injection; 70 mg/kg, 35 mg/kg; once daily) induces a significant antitumor activity and inhibited xenograft tumor progress as compared to treatment with vehicle[1].

Animal Model: NOD-SCID mice with MV4-11 cells[1]
Dosage: 70 mg/kg, 35 mg/kg
Administration: Intraperitoneal and intravenous injection; 70 mg/kg, 35 mg/kg; once daily
Result: Produced significant AML tumor inhibition rates of 93.5% at 70 mg/kg.
Molecular Weight

283.24

Formula

C₁₀H₁₃N₅O₅

CAS No.

1818-71-9

SMILES
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