| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| References | |
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| Additional Infomation |
SGR-1505, a MALT1 inhibitor, is an orally bioavailable mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) inhibitor with potential immunomodulatory and antitumor activities. After oral administration, SGR-1505 targets and inhibits MALT1 activity. This inhibits the MALT1-dependent CARD11-BCL10-MALT1 (CBM) signaling pathway, thereby suppressing the immunosuppressive function of regulatory T cells (Tregs) and upregulating the production of interferon-γ (IFN-γ) by Tregs in the tumor microenvironment (TME). This leads to inhibition of the Janus kinase/signal transduction and activating transcription factor (JAK/STAT) signaling pathway and the nuclear factor-κB (NF-κB) signaling pathway, inducing apoptosis and inhibiting tumor cell growth. MALT1 belongs to the caspase family of proteases and is an active component of the CBM signaling complex. It plays a crucial role in mediating the immunosuppressive activity of Treg cells and is overactivated in certain tumor cells, including non-Hodgkin's B-cell lymphoma.
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| Molecular Formula |
C18H12CLF4N9O
|
|---|---|
| Molecular Weight |
481.79
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| Exact Mass |
481.078
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| CAS # |
2661481-41-8
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| PubChem CID |
156539584
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| Appearance |
White to off-white solid powder
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| LogP |
2.9
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| tPSA |
106
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
33
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| Complexity |
759
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1=C(N2N=CC=N2)N=CC(=C1)NC(N1C2C=NC3=CC(=NN3C=2[C@](C)(C(F)(F)F)C1)F)=O
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| InChi Key |
DEMHKALZEXJNJH-QGZVFWFLSA-N
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| InChi Code |
InChI=1S/C18H12ClF4N9O/c1-17(18(21,22)23)8-30(11-7-24-13-5-12(20)29-31(13)14(11)17)16(33)28-9-4-10(19)15(25-6-9)32-26-2-3-27-32/h2-7H,8H2,1H3,(H,28,33)/t17-/m1/s1
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| Chemical Name |
(3R)-N-[5-chloro-6-(triazol-2-yl)pyridin-3-yl]-11-fluoro-3-methyl-3-(trifluoromethyl)-1,5,8,12-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),7,9,11-tetraene-5-carboxamide
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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 |
| 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) |
DMSO: ~100 mg/mL (~207.6 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (10.38 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 DMSO stock solution (50.0 mg/mL) to 900 μL of corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0756 mL | 10.3780 mL | 20.7559 mL | |
| 5 mM | 0.4151 mL | 2.0756 mL | 4.1512 mL | |
| 10 mM | 0.2076 mL | 1.0378 mL | 2.0756 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05544019
Conditions:Mature B-Cell Neoplasm|Non Hodgkin Lymphoma|DLBCL|Waldenstrom Macroglobulinemia|MALT Lymphoma|Follicular Lymphoma|Pediatric-Type Follicular Lymphoma|IRF4 Gene Rearrangement|EBV-Positive DLBCL, Nos|Burkitt Lymphoma|Plasmablastic Lymphoma|High-grade B-cell Lymphoma|Primary Cutaneous Follicle Center Lymphoma|Primary Effusion Lymphoma|Mantle Cell Lymphoma|DLBCL Germinal Center B-Cell Type|Primary Mediastinal Large B Cell Lymphoma|T-Cell/Histiocyte Rich Lymphoma|ALK-Positive Large B-Cell Lymphoma|Primary Cutaneous Diffuse Large B-Cell Lymphoma|Splenic Marginal Zone Lymphoma|Chronic Lymphocytic Leukemia|Nodal Marginal Zone Lymphoma|HHV8-Positive DLBCL, Nos|Lymphoplasmacytic Lymphoma|Duodenal-Type Follicular Lymphoma