WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 201530
CAS#: 204205-90-3
Description: Indibulin is a synthetic small molecule with antimitotic and potential antineoplastic activities. Indibulin binds to a site on tubulin that is different from taxane- or Vinca alkaloid-binding sites, destabilizing tubulin polymerization and inducing tumor cell cycle arrest and apoptosis. This agent has been shown to be active against multidrug-resistant (MDR) and taxane- resistant tumor cell lines. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
MedKoo Cat#: 201530
Name: Indibulin
CAS#: 204205-90-3
Chemical Formula: C22H16ClN3O2
Exact Mass: 389.0931
Molecular Weight: 389.83
Elemental Analysis: C, 67.78; H, 4.14; Cl, 9.09; N, 10.78; O, 8.21
Synonym: ZIO-301；ZERO/005632；ZINC01996564；d-24851; D-24851；NCGC00160428-01.
IUPAC/Chemical Name: 2-(1-(4-chlorobenzyl)-1H-indol-3-yl)-2-oxo-N-(pyridin-4-yl)acetamide
InChi Key: SOLIIYNRSAWTSQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H16ClN3O2/c23-16-7-5-15(6-8-16)13-26-14-19(18-3-1-2-4-20(18)26)21(27)22(28)25-17-9-11-24-12-10-17/h1-12,14H,13H2,(H,24,25,28)
SMILES Code: O=C(NC1=CC=NC=C1)C(C2=CN(CC3=CC=C(Cl)C=C3)C4=C2C=CC=C4)=O
Appearance: Solid powder
Purity: >98%
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 389.83 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Putey A, Popowycz F, Do QT, Bernard P, Talapatra SK, Kozielski F, Galmarini CM, Joseph B. Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies. J Med Chem. 2009 Oct 8;52(19):5916-25. PubMed PMID: 19743863.
Indibulin (ZIO-301) is a novel anti-cancer agent that binds to tubulin, one of the essential proteins for chromosomal segregation, and targets mitosis like the taxanes and Vinca alkaloids. It is available as both an oral and an intravenous form. Indibulin has a pharmacologic profile that is different from other tubulin inhibitors currently on the market. Indibulin binds to a site on tubulin that is different from the taxanes or Vinca alkaloid binding sites. In contrast to taxanes, which stabilize tubulin polymers, indibulin destabilizes tubulin polymerization. Indibulin has demonstrated significant and broad anti-tumor activity in many types of cancer cells. These include multi drug resistant tumor cell lines and taxane resistant tumor cell lines. In animal tumor models it was active at non-toxic levels in rat sarcoma AH13, MDR-1 leukemia mouse models and other xenograft models. No neurotoxicity or bone marrow suppression was detected at curative levels in animals. (Source: http://www.ziopharm.com/clinical_zio301.php ).
