Crotonoside

SKU: orb1222593

Description

Crotonoside has much more active than adenosine in reducing the blood pressure in rabbits and cats, in decreasing the tone of isolated intestinal strips of the rabbit, guinea pig and hamster and in stimulating the isolated uterus of guinea pigs and hamsters. Crotonoside inhibits the growth of S-18 and Ehrlich solid tumor in mice at the optimal doses of 96 mg/kg/day x 12 and 48 mg/kg/day x 12, with 1-T/C values of 65% and 6%, respectively.

Key Properties

• CAS Number: 1818-71-9
• MW: 283.24
• Purity: >98% (HPLC)
• Formula: C₁₀H₁₃N₅O₅
• SMILES: C1=NC2=C(NC(=O)N=C2N1C3C(C(C(O3)CO)O)O)N
• Target: Others
• Solubility: In Vitro: DMSO : 25 mg/mL (88.26 mM)

Bioactivity

• 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. Animal model: NOD-SCID mice with MV4-11 cells. 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.
• 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. Crotonoside (0-100 μM; 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. 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. 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. Cell Viability Assay 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. 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 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 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

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