| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Other Sizes |
Purity: ≥98%
| Targets |
VEGFR1
Met (HGFR, hepatocyte growth factor receptor); VEGFR (vascular endothelial growth factor receptor); gasdermin D. SCR-1481B1 is an inhibitor of HGFR (Met) and VEGFR kinases. It suppresses gasdermin D-mediated pyroptosis via targeting of the oligomerization interface. Met is a receptor tyrosine kinase involved in cell growth, survival, and migration, and is frequently dysregulated in cancer. VEGFR is a receptor tyrosine kinase involved in angiogenesis. |
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| ln Vitro |
BMS-794833, the active component of BMS-817378, with an IC50 of 1.7 nM/15 nM, is a strong ATP competitive inhibitor of Met/VEGFR2. It also has an IC50 of less than 3 nM for Ron, Axl, and Flt3. With an IC50 of 39 nM, BMS-794833 also suppresses the Met receptor-activated gastric carcinoma cell line, GTL-16./p> |
| ln Vivo |
BMS-798433 exhibits more than 50% TGI for at least one tumor doubling time in the GTL-16 human gastric tumor xenograft model, and no toxicity is seen over a 14-day period. In the U87 glioblastoma model, BMS-798433 likewise demonstrates total tumor stasis at 25 mg/kg. |
| Enzyme Assay |
BMS-794833, the active component of BMS-817378, has an IC50 of 1.7 nM/15 nM, making it a strong ATP competitive inhibitor of Met/VEGFR2. It also has an IC50 of <3 nM for Ron, Axl, and Flt3.
The kinase inhibition assay for SCR-1481B1 involves recombinant Met or VEGFR kinases incubated with ATP and a peptide substrate in the presence of varying concentrations of the compound. Kinase activity is measured by quantifying phosphorylated substrate using methods such as radioactive ATP incorporation, time-resolved fluorescence resonance energy transfer (TR-FRET), or luminescent kinase assays. IC₅₀ values are calculated from dose-response curves. For pyroptosis suppression, gasdermin D cleavage and pore formation are assessed. |
| Cell Assay |
Cancer cell lines dependent on Met activation (e.g., gastric cancer, lung cancer) or angiogenesis (e.g., endothelial cells) are cultured in appropriate medium. Cells are treated with increasing concentrations of SCR-1481B1 (typically ranging from 0.1 to 100 μM) for 48-72 hours. Cell viability is assessed using MTT, CCK-8, or CellTiter-Glo assays. Met and VEGFR signaling is assessed by Western blotting for phosphorylated receptors and downstream effectors.
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| Animal Protocol |
25mg/kg | U87 glioblastoma model.
| ADME/Pharmacokinetics |
SCR-1481B1 has a molecular weight of 699.98 g/mol and a molecular formula of C₂₈H₂₉ClF₂N₅O₁₀P. Detailed pharmacokinetic parameters are not extensively published. As a small molecule, SCR-1481B1 is expected to be orally bioavailable. The compound is typically stored as a powder at -20°C. Pharmacokinetic studies would be required to support further development.
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| Toxicity/Toxicokinetics |
Detailed toxicology data for SCR-1481B1 are limited in publicly available sources. As a multi-target kinase inhibitor, the compound's toxicity profile may include effects associated with inhibition of Met and VEGFR in normal tissues. Standard preclinical safety evaluation would be required for further development. The compound has shown activity in a mouse model of sepsis.
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| References | |
| Additional Infomation |
SCR-1481B1 (c-Met inhibitor 2) is a potent compound with activity against cancers dependent on Met activation and as a VEGFR inhibitor. It potently suppresses gasdermin D-mediated pyroptosis and is active in vivo in a mouse model of sepsis. The compound has a molecular formula of C₂₈H₂₉ClF₂N₅O₁₀P and a molecular weight of 699.98 g/mol. SCR-1481B1 represents a promising multi-target therapeutic agent for cancer and inflammatory diseases.
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| Molecular Formula |
C28H29CLF2N5O10P
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|---|---|
| Molecular Weight |
699.980933904648
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| Exact Mass |
699.13
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| Elemental Analysis |
C, 50.18; H, 4.75; Cl, 4.78; F, 5.12; N, 9.44; O, 21.56; P, 4.17
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| CAS # |
1174161-86-4
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| Related CAS # |
1174161-86-4 (tris);1174161-69-3;
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| PubChem CID |
119081412
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
47
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| Complexity |
1080
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C2=CN(C=C(C2=O)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F)COP(=O)(O)O)F.C(C(CO)(CO)N)O
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| InChi Key |
SDCKZXWUASKHNF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H18ClF2N4O7P.C4H11NO3/c25-21-20(7-8-29-23(21)28)38-19-6-5-15(9-18(19)27)30-24(33)17-11-31(12-37-39(34,35)36)10-16(22(17)32)13-1-3-14(26)4-2-13;5-4(1-6,2-7)3-8/h1-11H,12H2,(H2,28,29)(H,30,33)(H2,34,35,36);6-8H,1-3,5H2
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| Chemical Name |
[3-[[4-(2-amino-3-chloropyridin-4-yl)oxy-3-fluorophenyl]carbamoyl]-5-(4-fluorophenyl)-4-oxopyridin-1-yl]methyl dihydrogen phosphate;2-amino-2-(hydroxymethyl)propane-1,3-diol
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| Synonyms |
BMS-817378; BMS 817378; BMS817378; SCR-1481B1; SCR 1481B1; SCR1481B1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4286 mL | 7.1431 mL | 14.2861 mL | |
| 5 mM | 0.2857 mL | 1.4286 mL | 2.8572 mL | |
| 10 mM | 0.1429 mL | 0.7143 mL | 1.4286 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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