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.
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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: 99.95%
- CAS 番号: 1174161-86-4
- 分子式: C32H40ClF2N6O13P
- 分子量:821.12
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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生物活性
製品説明
IC50 & Target
[1]|
IL-1β |
VEGFR2 |
体外実験
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.
体内実験
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.
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Animal Model:C57BL/6J (8-12-week-old male, LPS-induced sepsis model)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose; administered 4 hours prior to LPS challenge
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Result:Reduced LPS-induced mortality to approximately 20%.
Strongly decreased serum levels of IL-1β, IL-6, and TNF-α at 12 hours after LPS challenge.
Did not further suppress inflammatory cytokine secretion in GSDMD-deficient septic mice.
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Animal Model:C57BL/6J (8-12-week-old male, E. coli-induced sepsis model)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Significantly improved the survival of E. coli-induced septic mice.
Reduced serum levels of IL-1β, IL-6, and TNF-α compared to vehicle controls, though to a lesser extent than with compound 98.
Did not significantly reduce bacterial colony counts in the spleen or liver relative to vehicle controls.
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Animal Model:C57BL/6J (8-12-week-old male, subcutaneous B16F10 melanoma model); Gsdmd-/- (8-12-week-old male, subcutaneous B16F10 melanoma model)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every other day; starting after tumor implantation
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Result:Reduced tumor burden and volume, and improved mouse survival, compared to anti-PD-L1 monotherapy.
Significantly increased the percentages and numbers of tumor-infiltrating CD4+ and CD8+ T cells.
Increased levels of IFN-γ, TNF-α, and granzyme B in tumor CD8+ T cells.
Decreased expression of exhaustion markers TIM-3 and TIGIT in CD8+ T cells.
Increased percentages and numbers of APCs including DCs and MHCII+ macrophages.
Still boosted antitumor immunity when combined with anti-PD-L1 in GSDMD-deficient mice.
化学情報
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CAS 番号 1174161-86-4
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性状 Solid
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分子量 821.12
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分子式 C32H40ClF2N6O13P
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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(C(F)=C3)OC4=C(Cl)C(N)=NC=C4.OCC(CO)(CO)N.OCC(CO)(CO)N
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別名
Metatinib anhydrous; c-Met inhibitor 2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外:
DMSO : ≥ 100 mg/mL (121.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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). 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). 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)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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). 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 | 1.2178 mL | 6.0892 mL | 12.1785 mL | 30.4462 mL |
| 5 mM | 0.2436 mL | 1.2178 mL | 2.4357 mL | 6.0892 mL | |
| 10 mM | 0.1218 mL | 0.6089 mL | 1.2178 mL | 3.0446 mL | |
| 15 mM | 0.0812 mL | 0.4059 mL | 0.8119 mL | 2.0297 mL | |
| 20 mM | 0.0609 mL | 0.3045 mL | 0.6089 mL | 1.5223 mL | |
| 25 mM | 0.0487 mL | 0.2436 mL | 0.4871 mL | 1.2178 mL | |
| 30 mM | 0.0406 mL | 0.2030 mL | 0.4059 mL | 1.0149 mL | |
| 40 mM | 0.0304 mL | 0.1522 mL | 0.3045 mL | 0.7612 mL | |
| 50 mM | 0.0244 mL | 0.1218 mL | 0.2436 mL | 0.6089 mL | |
| 60 mM | 0.0203 mL | 0.1015 mL | 0.2030 mL | 0.5074 mL | |
| 80 mM | 0.0152 mL | 0.0761 mL | 0.1522 mL | 0.3806 mL | |
| 100 mM | 0.0122 mL | 0.0609 mL | 0.1218 mL | 0.3045 mL |
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