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.
Product information
CAS Number: 1818-71-9
Molecular Weight: 283.24
Formula: C10H13N5O5
Chemical Name: 6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-3,9-dihydro-2H-purin-2-one
Smiles: NC1=NC(=O)NC2=C1N=CN2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
InChiKey: MIKUYHXYGGJMLM-UUOKFMHZSA-N
InChi: InChI=1S/C10H13N5O5/c11-7-4-8(14-10(19)13-7)15(2-12-4)9-6(18)5(17)3(1-16)20-9/h2-3,5-6,9,16-18H,1H2,(H3,11,13,14,19)/t3-,5-,6-,9-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 25 mg/mL (88.26 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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 (0-100μM; 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. 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.
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.
Products are for research use only. Not for human use.
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