Erastin,571203-78-6

Cat.No.:

IC-0127741

Product Information

Biological Activity

Erastin is a ferroptosis inducer. Erastin binds and inhibits voltage-dependent anion channels (VDAC2/VDAC3)[1].Erastin triggers oxidative, iron-dependent cell death. Treatment of NRAS-mutant HT-1080 fibrosarcoma cells with the RSL molecule erastin (10 µM) results in a time-dependent increase in cytosolic and lipid ROS beginning at 2 hours[1]. Cell death triggered by erastin is significantly inhibited by antioxidants (e.g., ¦Á-tocopherol, butylated hydroxytoluene, and ¦Â-carotene) and iron chelators, suggesting that ROS- and iron-dependent signaling is required for erastin-induced ferroptosis. Erastin can directly bind to VDAC2/3 in BJeLR cells. Knockdown of VDAC2 and VDAC3, but not VDAC1, leads to erastin resistance. Erastin has the ability to reduce glutathione level by directly inhibiting cystine/glutamate antiporter system Xc− activity, with activation of the ER stress response[2]. Erastin potently inhibits HT-29 cell survival. Erastin shows a dose-dependent effect, and 30 ¦ÌM of erastin displays the most dramatic effect[3].Intraperitoneal injection of erastin at well-tolerated doses dramatically inhibits HT-29 xenograft growth in severe combined immunodeficient mice[3].

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species

Mouse

Rat

Rabbit

Guinea pig

Hamster

Dog

Weight (kg)

0.02

0.15

1.8

0.4

0.08

10

Body Surface Area (m2)

0.007

0.025

0.15

0.05

0.02

0.5

Km factor

3

6

12

8

5

20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by  (Animal B Km / Animal A Km)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Order Information

Quantity

Price($£©

Price(€)

Price(£¤/CNY£©

Price(£¤/JYP£©

1mg

$60.00

€72.00

£¤600.00

¥11,940.00

5mg

$120.00

€144.00

£¤1,200.00

¥23,880.00

50mg

$450.00

€540.00

£¤4,500.00

¥89,550.00

Free Delivery on orders over $350.00.

Chemical Information

Molecular Weight

547.04

Formula

C30H31ClN4O4

CAS Number

571203-78-6

Purity

>98%

Solubility

DMSO : 12.5 mg/mL (22.85 mM; Need ultrasonic)  H2O : < 0.1 mg/mL (insoluble)

Storage

at -20¡ãC

Reference

[1]. Dixon SJ, et al. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012 May 25;149(5):1060-72.
[2]. Xie Y, et al. Ferroptosis: process and function. Cell Death Differ. 2016 Mar;23(3):369-79.
[3]. Huo H, et al. Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells. PLoS One. 2016 May 12;11(5):e0154605.

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