Crolibulin

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:

1. Kalmuk J, et al. Multimodal imaging guided preclinical trials of vascular targeting in prostate cancer. Oncotarget. 2015 Sep 15;6(27):24376-92.
2. 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.
3. 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.