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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.9%
- CAS No.: 2268739-68-8
- 화학식: C15H14FN3O
- 분자량:271.29
-
보관: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]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
Biological Activity
|
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.
-
Animal Model:Nemofl/fl Villin.creERT2 (both sexes, NEMO deletion induced via tamoxifen administration)[1]
-
Dosage:1 mg/kg; 5 mg/kg; 15 mg/kg; 50 mg/kg
-
Administration:p.o.; twice daily; 5 days
-
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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 2268739-68-8
-
Appearance Solid
-
분자량 271.29
-
화학식 C15H14FN3O
-
Color White to off-white
-
SMILES
F[C@@H]1C2=NC(C(C3CC3)=O)=NN2[C@H](C4=CC=CC=C4)C1
-
Synonyms
GDC-8264
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
-
Data Sheet (279 KB)
-
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)
-
Handling Instructions (2659 KB)
References
[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 Related Classifications
HY-152846 Related Classifications
Powered by Bioz