2. Apoptosis Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. Pyroptosis Interleukin Related c-Met/HGFR VEGFR
  4. SCR-1481B1

SCR-1481B1  (Synonyms: Metatinib anhydrous; c-Met inhibitor 2)

Cat. No.: HY-18711A Purity: 99.95%
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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.

SCR-1481B1

SCR-1481B1 Chemical Structure

CAS No. : 1174161-86-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Other Forms of SCR-1481B1:

SCR-1481B1 Related Antibodies

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

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[1][2][3][4].

IC50 & Target[1]

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.

SCR-1481B1 Related Antibodies
In Vivo

SCR-1481B1 (10 mg/kg; i.p.; single dose; administered 4 hours prior to LPS challenge) reduces LPS-induced sepsis mortality to ~20% and lowers serum inflammatory cytokine levels in wild-type mice by targeting GSDMD[1].
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.

Animal Model: C57BL/6J (8-12-week-old male, LPS-induced sepsis model)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose; administered 4 hours prior to LPS challenge
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.
Animal Model: C57BL/6J (8-12-week-old male, E. coli-induced sepsis model)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose
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.
Animal Model: C57BL/6J (8-12-week-old male, subcutaneous B16F10 melanoma model); Gsdmd-/- (8-12-week-old male, subcutaneous B16F10 melanoma model)[1]
Dosage: 10 mg/kg
Administration: i.p.; every other day; starting after tumor implantation
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.
Molecular Weight

821.12

Formula

C32H40ClF2N6O13P
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2178 mL 6.0892 mL 12.1785 mL
5 mM 0.2436 mL 1.2178 mL 2.4357 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 (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.

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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:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.95%

SDS (393 KB)

COA (258 KB) HNMR (300 KB) LCMS (87 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 (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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SCR-1481B1 Related Classifications

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  • 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:

SCR-1481B11174161-86-4Metatinib c-Met inhibitor 2PyroptosisInterleukin Relatedc-Met/HGFRVEGFRILVascular endothelial growth factor receptorHEK293T cellsiBMDMsanti-PD-L1 antibodyGSDMD-NTGasdermin DsepsispyroptosisTHP-1 monocytesmelanomaB16F10Inhibitorinhibitorinhibit

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