Description
Crolibulin (EPC2407) is a tubulin polymerization inhibitor, with potent apoptosis induction and cell growth inhibition. Crolibulin has anti-tumor activity. Crolibulin also has cardiovascular toxicity and neurotoxicity.
Product information
CAS Number: 1000852-17-4
Molecular Weight: 417.26
Formula: C18H17BrN4O3
Synonym:
EPC2407
Chemical Name: (4R)-2, 7, 8-triamino-4-(3-bromo-4, 5-dimethoxyphenyl)-4H-chromene-3-carbonitrile
Smiles: COC1=CC(=CC(Br)=C1OC)[C@H]1C(C#N)=C(N)OC2=C1C=CC(N)=C2N
InChiKey: JXONINOYTKKXQQ-CQSZACIVSA-N
InChi: InChI=1S/C18H17BrN4O3/c1-24-13-6-8(5-11(19)17(13)25-2)14-9-3-4-12(21)15(22)16(9)26-18(23)10(14)7-20/h3-6,14H,21-23H2,1-2H3/t14-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (299.57 mM; Need ultrasonic and warming)
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: ≥360 days 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:
Crolibulin shows significant cytotoxic activity against HT-29 cells, with an IC50 of 0.52 μM. Crolibulin is active against various experimental tumors and exhibit potent inhibition of mitosis at the G2/M stage.
References:
- Kalmuk J, et al. Multimodal imaging guided preclinical trials of vascular targeting in prostate cancer. Oncotarget. 2015 Sep 15;6(27):24376-92.
- Zhai X, et al. Discovery and Optimization of Novel 5-Indolyl-7-arylimidazo[1,2-a]pyridine-8-carbonitrile Derivatives as Potent Antitubulin Agents Targeting Colchicine-binding Site. Sci Rep. 2017 Feb 27;7:43398.
- S. P. Anthony, et al. EPC2407, a new beta-tubulin vascular disrupting agent with potent apoptosis and cell growth inhibition. Journal of Clinical Oncology 25, no. 18_suppl (June 20, 2007) 14043-14043.
Products are for research use only. Not for human use.
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