Indibulin CAS: 204205-90-3
MF: C22H16ClN3O2
MW: 389.83
A microtubule destabilizer.

Indibulin (CAS 204205-90-3)

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Synonym: D-24851
Application: A microtubule destabilizer
CAS Number: 204205-90-3
Molecular Weight: 389.83
Molecular Formula: C22H16ClN3O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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Indibulin is a microtubule destabilizer that blocks tubulin polymerization (IC50 = 0.3 μM). It acts by blocking cell cycle progression at metaphase and displays antitumor activity against a variety of malignancies in vitro (IC50 values ranging from 0.036-0.285 μM). Has been shown to induce complete tumor remission in the Yoshida AH13 rat sarcoma model in vivo. It is not neurotoxic due to an ability to discriminate between posttranslationally modified tubulin in mature neuronal microtubules and less-modified tubulin present in immature neuronal or nonneuronal microtubules. Also, Indibulin displays oral availability and efficacy towards MDR tumor cells.


References

1. Bacher, G. et al. 2001. Cancer Res. 61(1): 392-399. PMID: 11196193
2. Ito, H. et al. 2005. Int. J. Oncol. 26(3): 589-596. PMID: 15703812
3. Wienecke, A. and Bacher, G. 2009. Cancer Res. 69(1): 171-177. PMID: 19118000

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mM).
Storage :
Desiccate at -20° C
Density :
1.31 g/cm3
Refractive Index :
n20D 1.66
IC50 :
blocks tubulin polymerization: IC50 = 0.3 µM (rat); HT-29 (Colon adenocarcinoma cells): IC50 = 72 nM (human); MDA-MB-231 (Breast adenocarcinoma cells): IC50 = 74 nM (human); SK-OV-3 (Ovarian carcinoma cells): IC50 = 77 nM (human); P388 (Lymphoma cells): IC50 = 77 nM (mouse); NUGC-3 (Gastric carcinoma cells): IC50 = 524 nM (human)
pK Values :
pKa: 9.38 (Predicted), pKb: 4.86 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
2929
MDL Number :
MFCD05861105
SMILES :
C1=CC=C2C(=C1)C(=CN2CC3=CC=C(C=C3)Cl)C(=O)C(=O)NC4=CC=NC=C4

Download SDS (MSDS)

Certificate of Analysis

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