| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
SBP-3264 targets serine/threonine-protein kinases 3 and 4 (STK3 and STK4), also known as MST2 and MST1. These kinases are core components of the Hippo signaling pathway, which regulates organ size, tissue homeostasis, and tumor suppression. By blocking MST1/2, it prevents YAP/TAZ phosphorylation, sustaining their transcriptional repression and thereby curbing proliferation.
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| ln Vitro |
In vitro, SBP-3264 specifically inhibits the Hippo signaling pathway in cultured mammalian cells. It potently inhibits STK3 and STK4 with low-nanomolar activity. The compound's activity has been characterized in kinase inhibition assays using recombinant STK3 and STK4 proteins. It is used as a chemical probe to study the role of these kinases in cellular processes, including proliferation and survival.
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| ln Vivo |
In vivo, SBP-3264 possesses favorable pharmacokinetic and pharmacodynamic properties in mice. In AML models, SBP-3264 suppresses leukemic cell growth. By inhibiting these kinases, the compound can modulate Hippo signaling and affect tumor growth.
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| Enzyme Assay |
Non-cellular assays for SBP-3264 involve measuring its inhibitory activity against STK3 and STK4 kinases. This is typically done using recombinant proteins in an in vitro kinase assay that measures the phosphorylation of a substrate in the presence of ATP. The inhibition of this activity is used to determine the IC₅₀ value.
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| Cell Assay |
Cell-based assays for SBP-3264 involve studying its effects on Hippo signaling in cells. Cells can be treated with the compound, and the phosphorylation of downstream targets, such as YAP and TAZ, can be assessed by Western blot. The effects on cell proliferation, survival, and gene expression can also be measured.
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| Animal Protocol |
In vivo animal experiments with SBP-3264 would typically involve administering the compound to mice to study its effects in disease models. Xenograft models of acute myeloid leukemia (AML) could be used to evaluate its anti-tumor efficacy. Pharmacokinetic and toxicity studies would also be conducted to assess its suitability for further development.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for SBP-3264 indicate that it possesses favorable pharmacokinetic and pharmacodynamic properties in mice. The compound is soluble in DMSO at 55 mg/mL. It can be formulated for in vivo use in 10% DMSO+40% PEG300+5% Tween 80+45% Saline at 1 mg/mL.
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| Toxicity/Toxicokinetics |
No specific toxicity data have been reported for SBP-3264. As a research compound, it should be handled with standard laboratory safety precautions.
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| References | |
| Additional Infomation |
SBP-3264 is a research compound, not an approved drug. It is a novel inhibitor of STK3 and STK4, which are core components of the Hippo signaling pathway. It is a valuable chemical probe for understanding the roles of these kinases in acute myeloid leukemia (AML).
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| Molecular Formula |
C19H20CLN5O
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|---|---|
| Molecular Weight |
369.848002433777
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| Exact Mass |
369.135
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| CAS # |
2869148-13-8
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| PubChem CID |
162366980
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.38±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
498
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=O)NC1CCN(CC1)C2=NC=NC3=C2C(=CN3)C4=CC(=CC=C4)Cl
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| InChi Key |
AYRVYPOFYQSRNH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20ClN5O/c1-12(26)24-15-5-7-25(8-6-15)19-17-16(10-21-18(17)22-11-23-19)13-3-2-4-14(20)9-13/h2-4,9-11,15H,5-8H2,1H3,(H,24,26)(H,21,22,23)
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| Chemical Name |
N-[1-[5-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]piperidin-4-yl]acetamide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 62.5 mg/mL (168.99 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 20.8 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: ≥ 2.08 mg/mL (5.62 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7038 mL | 13.5190 mL | 27.0380 mL | |
| 5 mM | 0.5408 mL | 2.7038 mL | 5.4076 mL | |
| 10 mM | 0.2704 mL | 1.3519 mL | 2.7038 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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