| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
ALK2-IN-4 targets ALK2 (activin receptor-like kinase 2), also known as ACVR1. ALK2 is a serine/threonine kinase that mediates signaling of the BMP (bone morphogenetic protein) pathway. This pathway is involved in a wide range of cellular processes, including bone formation, cell differentiation, and embryonic development. Dysregulation of ALK2 signaling is associated with conditions such as fibrodysplasia ossificans progressiva (FOP) and certain cancers.
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|---|---|
| ln Vitro |
In vitro, ALK2-IN-4 is a potent inhibitor of ALK2. Its inhibitory activity is typically assessed in cell-free kinase assays using recombinant ALK2 enzyme. By inhibiting ALK2, it can block BMP signaling, which can be confirmed by measuring the phosphorylation of downstream SMAD proteins.
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| ln Vivo |
In vivo data for ALK2-IN-4 is not provided in the available literature.
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| Enzyme Assay |
The ALK2 inhibitory activity of ALK2-IN-4 is assessed using in vitro kinase assays. Recombinant ALK2 kinase is incubated with a substrate and varying concentrations of the compound.
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| Cell Assay |
The cellular activity of ALK2-IN-4 is evaluated in cell lines with active BMP signaling. Cells are treated with the compound, and the phosphorylation of SMAD1/5/8 is measured by Western blot.
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| Animal Protocol |
In animal studies, ALK2-IN-4 would be administered to mice to study its effects on ALK2-mediated processes.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ALK2-IN-4 are not detailed.
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| Toxicity/Toxicokinetics |
No toxicology data is provided.
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| References | |
| Additional Infomation |
ALK2-IN-4 (CAS: 2248154-85-8) is a potent research tool for studying ALK2 kinase.
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| Molecular Formula |
C26H30FN7O
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|---|---|
| Molecular Weight |
475.561108112335
|
| Exact Mass |
475.249
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| CAS # |
2248154-85-8
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| Related CAS # |
KER047 succinate;2416307-25-8
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| PubChem CID |
142464264
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| Appearance |
Light yellow to yellow solid powder
|
| LogP |
2.8
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
35
|
| Complexity |
701
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC1C(=CC2C(C=1)=NC=CC=2C1C=NN2C=1N=CC(=C2)N1CCC(CC1)N1CCN(C)CC1)OC
|
| InChi Key |
UYQADNMBNQEQQG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H30FN7O/c1-31-9-11-33(12-10-31)18-4-7-32(8-5-18)19-15-29-26-22(16-30-34(26)17-19)20-3-6-28-24-14-23(27)25(35-2)13-21(20)24/h3,6,13-18H,4-5,7-12H2,1-2H3
|
| Chemical Name |
7-fluoro-6-methoxy-4-[6-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline
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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)
|
| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~21.03 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.10 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (2.10 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 10.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1028 mL | 10.5139 mL | 21.0278 mL | |
| 5 mM | 0.4206 mL | 2.1028 mL | 4.2056 mL | |
| 10 mM | 0.2103 mL | 1.0514 mL | 2.1028 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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