2. Apoptosis Immunology/Inflammation
  3. RIP kinase Interleukin Related
  4. Flizasertib

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.

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Flizasertib

Flizasertib Chemical Structure

CAS No. : 2268739-68-8

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Based on 1 publication(s) in Google Scholar

Flizasertib Related Antibodies

Top Publications Citing Use of Products

View All RIP kinase Isoform Specific Products:

View All Isoforms
RIPK1 RIPK2 RIPK3

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View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target[1]

hRIP1

0.00071 μM (Ki app)

Cynomolgus RIP1

0.0013 μM (Ki app)

IL-1β

 

In Vitro

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.

Flizasertib Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUC
Rat[1] 5 mg/kg p.o. 20.2 μM 110 μM·h
Mice[1] 5 mg/kg p.o. 61.9 μM 242 μM·h
Dog[1] 5 mg/kg p.o. 3.36 μM 15.6 μM·h
Cynomolgus Monkey[1] 5 mg/kg p.o. 17.1 μM 71.9 μM·h
In Vivo

GDC-8264 (1-50 mg/kg; p.o.; twice daily; 5 days) provides dose-dependent protection against NEMO deletion-induced colitis and ileitis in mice[1].

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).
Clinical Trial
Molecular Weight

271.29

Formula

C15H14FN3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

F[C@@H]1C2=NC(C(C3CC3)=O)=NN2[C@H](C4=CC=CC=C4)C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6861 mL 18.4305 mL 36.8609 mL
5 mM 0.7372 mL 3.6861 mL 7.3722 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.9%

SDS (254 KB)

COA (256 KB) HNMR (180 KB) CNMR (180 KB) LCMS (109 KB)

Handling Instructions (2659 KB)
References

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
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Flizasertib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Flizasertib2268739-68-8GDC-8264GDC8264GDC 8264RIP kinaseInterleukin RelatedReceptor-interacting protein kinasesRIPKILnecroptosiscynomolgus monkeymouseHT29 cellsratMAPKRIP1L929 cellsNF-κBH9c2 cellsInhibitorinhibitorinhibit

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