Flizasertib
Based on 1 Customer Validation
Flizasertib (GDC-8264) is an orally active, reversible and selective RIP1 inhibitor with Kiapp values of 0.00071 μM and 0.0013 μM for human and cynomolgus monkey RIP1 kinase, respectively. Flizasertib blocks RIP1 autophosphorylation but does not affect RIP1 protein stability. Flizasertib inhibits pro-inflammatory cytokines (CCL3, CCL4, and IL-1β) production. Flizasertib results in inhibition of colitis and ileitis. Flizasertib can be used in the research of cardiac surgery-associated acute kidney injury.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.9%
- CAS 番号: 2268739-68-8
- 分子式: C15H14FN3O
- 分子量:271.29
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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hRIP1 0.00071 μM (Ki app) |
Cynomolgus RIP1 0.0013 μM (Ki app) |
IL-1β |
Flizasertib (0.26 nM to 10,000 nM) potently inhibits human and cynomolgus monkey RIP1 kinase activity with Kiapp values of 0.00071 μM and 0.0013 μM, respectively[1].
Flizasertib exhibits high selectivity for RIP1, with a Kd of 0.0031 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nemofl/fl Villin.creERT2 (both sexes, NEMO deletion induced via tamoxifen administration)[1]
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Dosage:1 mg/kg; 5 mg/kg; 15 mg/kg; 50 mg/kg
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Administration:p.o.; twice daily; 5 days
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Result:Almost completely protected NEMO-deficient intestines from colitis and ileitis (50 mg/kg).\nProvided significant protection against colitis and ileitis (15 mg/kg, 5 mg/kg).\nExerted a modest protective effect in the colon but not in the ileum (1 mg/kg).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2268739-68-8
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性状 Solid
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分子量 271.29
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分子式 C15H14FN3O
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Color White to off-white
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SMILES
F[C@@H]1C2=NC(C(C3CC3)=O)=NN2[C@H](C4=CC=CC=C4)C1
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別名
GDC-8264
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 10 mg/mL (36.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Patel S, et al. Discovery of Clinical Candidate GDC-8264, a Novel, Potent and Selective RIP1 Inhibitor for Amelioration of Tissue Damage and the Treatment of Inflammatory Diseases. J Med Chem. 2025;68(21):23050-23077. [Content Brief]
[2]. Jones NS, et al. A phase I, randomized, ascending-dose study to assess safety, pharmacokinetics, and activity of GDC-8264, a RIP1 inhibitor, in healthy volunteers. Clin Transl Sci. 2023;16(10):1997-2009. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6861 mL | 18.4305 mL | 36.8609 mL | 92.1523 mL |
| 5 mM | 0.7372 mL | 3.6861 mL | 7.3722 mL | 18.4305 mL | |
| 10 mM | 0.3686 mL | 1.8430 mL | 3.6861 mL | 9.2152 mL | |
| 15 mM | 0.2457 mL | 1.2287 mL | 2.4574 mL | 6.1435 mL | |
| 20 mM | 0.1843 mL | 0.9215 mL | 1.8430 mL | 4.6076 mL | |
| 25 mM | 0.1474 mL | 0.7372 mL | 1.4744 mL | 3.6861 mL | |
| 30 mM | 0.1229 mL | 0.6143 mL | 1.2287 mL | 3.0717 mL |
Flizasertib 関連分類
HY-152846 関連分類
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