| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
YES1, IRAK1, LYN, and other kinases.
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|---|---|
| ln Vitro |
SB1-G-187 is a multi-kinase degrader. It has been shown to induce potent degradation of YES1, IRAK1, and LYN in cells. It mediates degradation in a manner that is partially dependent on the p97/VCP pathway. In vitro studies have also demonstrated its ability to degrade additional kinases. The compound is a click chemistry reagent, as it contains an alkyne group that can be used for further conjugation.
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| ln Vivo |
No specific in vivo activity has been reported for SB1-G-187; however, as a PROTAC degrader targeting multiple kinases, it is expected to have in vivo efficacy in animal models of cancer and inflammation. Such studies are currently ongoing for this research compound.
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| Enzyme Assay |
N/A; as a complete PROTAC molecule, its binding to target kinases and to an E3 ubiquitin ligase (cereblon) is typically assessed using biophysical methods such as surface plasmon resonance (SPR) or fluorescence polarization (FP) to determine binding affinities. Functional target engagement is then confirmed via degradation assays.
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| Cell Assay |
The in vitro degradation activity of SB1-G-187 is evaluated in kinase-expressing cancer cell lines. Cells are treated with increasing concentrations of the compound (e.g., 1 nM to 10 uM) for a defined period, typically 4-24 hours. After treatment, cell lysates are prepared and the levels of specific target kinases (e.g., YES1, IRAK1, LYN) are measured by Western blotting or quantitative proteomics.
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| Animal Protocol |
N/A; in vivo efficacy studies for SB1-G-187 would typically be conducted in mouse xenograft models of kinase-driven cancers. The compound would be formulated in a suitable vehicle (e.g., 10% DMSO, 40% PEG300, 5% Tween-80, 45% saline) and administered via oral gavage, IP, or IV injection. Tumor growth inhibition, target protein degradation in tumor tissue, and overall animal health would be monitored.
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| ADME/Pharmacokinetics |
SB1-G-187 has a molecular weight of 1022.03, a molecular formula of C52H54F3N9O10, and a purity of >98%. It is typically stored as a solid powder at -20degC for up to 3 years, protected under nitrogen, or in a solvent at -80degC for 6 months or at -20degC for 1 month. It is soluble in DMSO at 100 mg/mL.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not for human therapeutic or clinical use. Standard safe handling practices for laboratory chemical reagents should be followed. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.
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| References | |
| Additional Infomation |
SB1-G-187 represents a novel multi-kinase degradation approach, targeting multiple nodes within a signaling pathway simultaneously. This strategy may offer advantages over selective single-target inhibitors by potentially overcoming resistance mechanisms and providing more robust pathway inhibition. The compound contains an alkyne group for click chemistry, enabling further functionalization for pull-down assays or probe development.
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| Molecular Formula |
C52H54F3N9O10
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|---|---|
| Molecular Weight |
1022.0346827507
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| Exact Mass |
1021.394
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| CAS # |
2769753-18-4
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| PubChem CID |
163196234
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| Appearance |
White to light yellow solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
74
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| Complexity |
2020
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=C(C=C1)C(=O)NC2=CC(=C(C=C2)CN3CCN(CC3)CCCOCCOCCOCCNC(=O)COC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O)C(F)(F)F)C#CC7=CN=C8N7N=CC=C8
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| InChi Key |
HKRYQLKHNCVSRZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C52H54F3N9O10/c1-34-8-9-36(29-35(34)11-13-39-31-57-44-7-3-16-58-64(39)44)48(67)59-38-12-10-37(41(30-38)52(53,54)55)32-62-21-19-61(20-22-62)18-4-23-71-25-27-73-28-26-72-24-17-56-46(66)33-74-43-6-2-5-40-47(43)51(70)63(50(40)69)42-14-15-45(65)60-49(42)68/h2-3,5-10,12,16,29-31,42H,4,14-15,17-28,32-33H2,1H3,(H,56,66)(H,59,67)(H,60,65,68)
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| Chemical Name |
N-[4-[[4-[3-[2-[2-[2-[[2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetyl]amino]ethoxy]ethoxy]ethoxy]propyl]piperazin-1-yl]methyl]-3-(trifluoromethyl)phenyl]-3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methylbenzamide
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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 (e.g. under nitrogen), 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) |
DMSO :~100 mg/mL (~97.84 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (4.89 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (4.89 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 50.0 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 | 0.9784 mL | 4.8922 mL | 9.7844 mL | |
| 5 mM | 0.1957 mL | 0.9784 mL | 1.9569 mL | |
| 10 mM | 0.0978 mL | 0.4892 mL | 0.9784 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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