IKE
- Product Name
- IKE
- CAS No.
- 1801530-11-9
- Chemical Name
- IKE
- Synonyms
- IKE);PUN-30119;Ferroptosis inducer IKE;Imidazole ketone erastin;IKE(Imidazole ketone erastin);Imidazole ketone erastin (PUN30119);Imidazole ketone erastin, 10 mM in DMSO;Imidazole ketone erastin (PUN30119) ，S8877;Imidazole ketone erastin (Ferroptosis inducer IKE;IMIDAZOLE KETONE ERASTIN;FERROPTOSIS INDUCER IKE;IKE
- CBNumber
- CB04844901
- Molecular Formula
- C35H35ClN6O5
- Formula Weight
- 655.14
- MOL File
- 1801530-11-9.mol
IKE Property
- Boiling point:
- 886.5±75.0 °C(Predicted)
- Density
- 1.34±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMF: 10mg/mL,DMSO: 1mg/mL,DMSO:PBS (pH 7.2) (1:2): 0.25mg/mL
- form
- A crystalline solid
- pka
- 6.12±0.10(Predicted)
- color
- White to yellow
- InChIKey
- PSPXJPWGVFNGQI-UHFFFAOYSA-N
- SMILES
- N1C2=C(C=CC=C2)C(=O)N(C2=CC(C(CN3C=NC=C3)=O)=CC=C2OC(C)C)C=1CN1CCN(C(COC2=CC=C(Cl)C=C2)=O)CC1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 27088
- Product name
- Imidazole Ketone Erastin
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $93
- Updated
- 2024/03/01
- Product number
- 27088
- Product name
- Imidazole Ketone Erastin
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $298
- Updated
- 2024/03/01
- Product number
- 27088
- Product name
- Imidazole Ketone Erastin
- Packaging
- 10mg
- Price
- $502
- Updated
- 2024/03/01
- Product number
- DC22092
- Product name
- Imidazoleketoneerastin（IKE）
- Purity
- >98%
- Packaging
- 100mg
- Price
- $700
- Updated
- 2021/12/16
- Product number
- DC22092
- Product name
- Imidazoleketoneerastin（IKE）
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1200
- Updated
- 2021/12/16
IKE Chemical Properties,Usage,Production
Description
Imidazole ketone erastin is an inducer of ferroptosis. It inhibits glutamate release in human CCF-STTG1 astrocytoma cells (IC50 = 30 nM), indicating inhibition of the system xc- cystine/glutamate transporter. Imidazole ketone erastin increases production of lipid reactive oxygen species (ROS) in SUDHL6 diffuse large B cell lymphoma (DLBCL) cells in a concentration-dependent manner, as well as reduces glutathione (GSH) levels in these cells (IC50 = 34 nM). It inhibits the growth of HT-1080 fibrosarcoma cells (GI50 = 310 nM) as well as HRASG12V-overexpressing BJeLR cells (IC50 = 3 nM). Imidazole ketone erastin (23 and 40 mg/kg) reduces tumor growth in an SUDHL6 mouse xenograft model.
Uses
PUN30119 is potent, metabolically stable inhibitor of system xc.
in vivo
IKE (23-40 mg/kg; i.p. once daily for 13 d) inhibits tumor growth in mice[1].
IKE (50 mg/kg; a single i.p) depletes GSH significantly starting from 4 h, and increases in the relative abundance of free fatty acids, phospholipids, and diacylglycerols (DAG) in mice[1].
IKE (50 mg/kg) exhibits half-life (1.82, 1.31, and 0.96 h) and Cmax (19515, 11384, and 5203 ng/mL) following different administration (i.p., i.v., and p.o. respectively) in mice[1].
| Animal Model: | Male NCG mice bearing SUDHL6 subcutaneous xenografts[1] |
| Dosage: | 23, 40 mg/kg |
| Administration: | I.p. injection once daily for 13 days |
| Result: | Caused a significant decrease in tumor growth starting from day 9. Had a weight loss starting from day 9. |
| Animal Model: | NOD/SCID mice (12 weeks old; ~28 g weight)[1] |
| Dosage: | 50 mg/kg (Pharmacokinetic Analysis) |
| Administration: | A single i.p., i.v., and p.o. administration |
| Result: | I.p.: T1/2=1.82 h, Cmax=19515 ng/mL. I.v.: T1/2=1.31 h, Cmax=11384 ng/mL. P.o.: T1/2=0.96 h, Cmax=5203 ng/mL. |
References
[1] YAN ZHANG . Imidazole Ketone Erastin Induces Ferroptosis and Slows Tumor Growth in a Mouse Lymphoma Model[J]. Cell Chemical Biology, 2019, 26 5: Pages 623-633.e9. DOI: 10.1016/j.chembiol.2019.01.008
[2] MARIE-HELENE LARRAUFIE . Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility[J]. Bioorganic & Medicinal Chemistry Letters, 2015, 25 21: Pages 4787-4792. DOI: 10.1016/j.bmcl.2015.07.018
[3] ZHIPENG LI. Ribosome stalling during selenoprotein translation exposes a ferroptosis vulnerability[J]. Nature chemical biology, 2022, 18 7: 751-761. DOI: 10.1038/s41589-022-01033-3
IKE Preparation Products And Raw materials
Raw materials
Preparation Products
IKE Suppliers
- Tel
- 13761310616
- Fax
- QQ: 39324283
- 39324283@qq.com
- Country
- China
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- 0411-62910999 13889544652
- sales@meilune.com
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- China
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- 021-58170097
- info@topbiochem.com
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- China
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- 9510
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- 18149758185
- sales-cpd@caerulumpharma.com
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- China
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- 3506
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- 15221275939
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- 021-50706099
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- China
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- 021-52996696，15000506266 15000506266
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- +86-21-52996696
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- China
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- 021-61312847; 18021002903
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- QQ:3008007432
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- China
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- QQ:2853530913
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- 021-31433387 15618786686
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- QQ:1369748377
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- China
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- 021-QQ：65489617 15618227136
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- 21-5161 9052
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