SCR-1481B1
Based on 1 Customer Validation
SCR-1481B1 (Metatinib anhydrous; c-Met inhibitor 2) is an inhibitor of the N-terminal fragment of Gasdermin D (GSDMD), with an IC50 of 1.04 μM and a Ka of 0.42 μM in mice. SCR-1481B1 effectively blocks GSDMD-NT oligomerization and pore formation, inhibits GSDMD-mediated pyroptosis (Pyroptosis), preserves mitochondrial integrity, and reduces proinflammatory cytokine secretion. SCR-1481B1 also inhibits angiogenesis, exerts GSDMD-independent antitumor effects, and enhances the infiltration of antitumor immune cells. SCR-1481B1 is also an inhibitor targeting to c-MET and VEGFR2, can be used in studies related to melanoma and sepsis.
For research use only. We do not sell to patients.
- Purity : 99.99%
- CAS No.: 1174161-69-3
- Formula: C24H18ClF2N4O7P
- Molecular Weight:578.85
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
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IL-1β |
VEGFR2 |
In Vitro
SCR-1481B1 (1-40 μM; 1 h pre-incubation) dose-dependently inhibits LPS plus nigericin-induced GSDMD-mediated pyroptosis in iBMDMs, reducing both LDH release and IL-1β secretion[1].
SCR-1481B1 (20 μM) inhibits LPS plus nigericin-induced GSDMD-mediated pyroptosis in human THP-1 monocytes, reducing both LDH release and IL-1β secretion[1].
SCR-1481B1 (20 μM; 4 h) inhibits mouse and human GSDMD-N oligomerization and subsequent pyroptotic cell death in HEK293T cells[1].
SCR-1481B1 (20 μM; 4 h) inhibits GSDMD oligomerization and pyroptotic cell death downstream of caspase-1/11-mediated GSDMD cleavage in HEK293T cells[1].
SCR-1481B1 (20 μM) inhibits human and mouse GSDMD-N oligomerization in the cytosol of HEK293T cells, as measured by split-luciferase reconstitution[1].
SCR-1481B1 (20 μM; 4 h pre-incubation) specifically binds to core sites at the oligomerization interface I of mouse GSDMD-N, enhancing its stability against protease degradation[1].
SCR-1481B1 (20 μM) directly binds to core sites at the oligomerization interface I of purified mouse GSDMD-N, increasing its thermal stability[1].
SCR-1481B1 (0.15-20 μM; 60 min) inhibits GSDMD-N-mediated liposome pore formation with an IC50 of 1.04 μM[1].
SCR-1481B1 (Metatinib) binds to the GSDMD dimer with a docking score of -7.28 kcal/mol[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SCR-1481B1 (10 mg/kg; i.p.; single dose) improves survival and reduces serum inflammatory cytokine levels in E. coli-induced septic mice, though it does not significantly reduce organ bacterial burden[1].
SCR-1481B1 (10 mg/kg; i.p.; every other day; starting after tumor implantation) enhances the antitumor efficacy of anti-PD-L1 antibody in a B16F10 melanoma model by increasing tumor-infiltrating immune cells and reducing T cell exhaustion, with activity independent of GSDMD[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- Human pluripotent stem cell endothelial-cell differentiation
- Vascular/Branching Fractal Analysis
- LPS-Induced Endotoxemia/Systemic Inflammation
- Endothelial Tube Formation Assay
- Research Protocol for Inflammation-related Diseases
- Endothelial Cell Migration/Angiogenic Sprouting Assay
- Pyroptosis Solutions
Chemical Information
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CAS No. 1174161-69-3
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Appearance Solid
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Molecular Weight 578.85
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Formula C24H18ClF2N4O7P
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Color White to off-white
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SMILES
O=C(C1=CN(COP(O)(O)=O)C=C(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C(Cl)C(N)=NC=C4)C(F)=C3
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Synonyms
Metatinib free base; c-Met inhibitor 2 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro:
DMSO : 4.55 mg/mL (7.86 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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)
Purity & Documentation
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Data Sheet (294 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Hu Y, et al. Identification of two repurposed drugs targeting GSDMD oligomerization interface I to block pyroptosis. Cell Chem Biol. 2024;31(12):2024-2038.e7. [Content Brief]
[3]. Lestari B, et al. Discovery of pyroptosis-inducing natural products in neuroblastomas: computational studies with experimental validation. BMC Complement Med Ther. 2025;25(1):279. Published 2025 Jul 19. [Content Brief]
[4]. Cheng K, et al. Safety, Efficacy, and Pharmacokinetics of Metatinib Tromethamine Tablet in Patients with Advanced Refractory Solid Tumors: A Phase I Clinical Trial. Oncologist. 2021 Aug;26(8):649-e1313. [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 (sealed storage, away from moisture and light). 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 | 1.7276 mL | 8.6378 mL | 17.2756 mL | 43.1891 mL |
| 5 mM | 0.3455 mL | 1.7276 mL | 3.4551 mL | 8.6378 mL |
SCR-1481B1 Related Classifications
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