ErastinA cell-permeable compound that exhibits oncogene-selective lethality in cells with H-Ras mutationa

Erastin (CAS 571203-78-6)

Erastin | CAS 571203-78-6 is rated 5.0 out of 5 by 1.
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Synonym: 2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-Quinazolinone
Application: A cell-permeable compound that exhibits oncogene-selective lethality in cells with H-Ras mutationa
CAS Number: 571203-78-6
Purity: ≥99%
Molecular Weight: 547.05
Molecular Formula: C30H31ClN4O4
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations. Erastin is shown to bind mitochondrial volatage-dependent anion channels (VDAC) and alter its gating; Erastin rapidly induces an oxidative, non-apoptotic cell death in several human tumors harboring activating mutations in the RAS-RAF-MEK signaling.


References

1. Yagoda, N., et al. 2007. Nature. 447: 864-868. PMID: 17568748

Physical State :
Solid
Solubility :
Soluble in DMSO (>10 mg/ml).
Storage :
Store at -20° C
Boiling Point :
721.94° C at 760 mmHg (Predicted)
Density :
1.29 g/cm3
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
BJ (Foreskin fibroblast cells): IC50 = 900 nM (human); HT-1080 (Fibrosarcoma cells): IC50 = 1.3 µM (human); BJ-TERT/LT/ST/RASV12 cells: EC5050 = 6.0 µM
pK Values :
pKb: 5.54 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
11214940
MDL Number :
MFCD09837984
SMILES :
CCOC1=CC=CC=C1N2C(=O)C3=CC=CC=C3N=C2C(C)N4CCN(CC4)C(=O)COC5=CC=C(C=C5)Cl

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Certificate of Analysis

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Rated 5 out of 5 by from Yagoda et al Yagoda et al. (PubMed ID 17568748) found that Erastin induced oxidative stress in cells with oncogenic RAS by binding to mitochondrial voltage-dependent anion channels (VDACs). -SCBT Publication Review
Date published: 2015-07-15
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