| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
Pim1/AKK1-IN-1 targets multiple serine/threonine kinases involved in various cellular processes. Its primary targets include Pim1, a kinase involved in cell survival and proliferation, and AKK1 (also known as AAK1), which plays a role in clathrin-mediated endocytosis. It also inhibits MST2, a key component of the Hippo signaling pathway, and LKB1, a tumor suppressor kinase. Its broad target profile makes it a useful tool for studying these pathways.
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| ln Vitro |
Pim1/AKK1-IN-1 is multiplex, having Kd values of 53 nM for AAK1 and 380 nM for LKB1 [1].
In vitro, Pim1/AKK1-IN-1 demonstrates potent inhibitory activity against its targets, with Kd values in the nanomolar range. By inhibiting Pim1 activity, it can suppress cancer cell growth, promote apoptosis, and enhance sensitivity to other anticancer therapies. Its multi-kinase inhibition profile suggests it could affect various signaling pathways simultaneously, making it a valuable tool for studying kinase biology in cancer. |
| ln Vivo |
In vivo, preclinical studies have demonstrated the potency of Pim1/AKK1-IN-1. While specific in vivo efficacy data are not detailed in the provided sources, its mechanism of inhibiting key kinases involved in cancer cell survival and proliferation supports its potential as an anticancer agent. It is used in research to study the effects of multi-kinase inhibition in animal models of cancer.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies for Pim1/AKK1-IN-1 are typically performed using kinase activity assays. In these assays, the recombinant kinase (e.g., Pim1, AKK1, MST2, LKB1) is incubated with its substrate and ATP in the presence of varying concentrations of the inhibitor. The enzyme's activity is measured by detecting the phosphorylation of the substrate. The Kd values, which are in the nanomolar range, are determined from these experiments, confirming the compound's high affinity for its targets.
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| Cell Assay |
In vitro cellular assays for Pim1/AKK1-IN-1 are used to study its effects on cancer cells. Cells are treated with the compound, and key readouts include cell viability (MTT or CellTiter-Glo assays), apoptosis (Annexin V/PI staining), and the phosphorylation status of downstream targets of the inhibited kinases (e.g., phospho-ERK, phospho-AKT). These assays are crucial for confirming the compound's mechanism of action and its potential as an anticancer agent.
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| Animal Protocol |
In vivo animal studies for Pim1/AKK1-IN-1 are not extensively detailed in the provided sources. However, based on its mechanism, it would be studied in xenograft models using cancer cell lines that are sensitive to the inhibition of its targets. Tumor-bearing mice would be treated with the compound, and endpoints would include tumor growth inhibition, survival, and pharmacodynamic analysis of target inhibition in the tumor tissue. Preclinical studies have demonstrated its potency.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Pim1/AKK1-IN-1 are characterized by its molecular weight of 339.35 g/mol and a molecular formula of C₂₀H₁₃N₅O. Its solubility is not detailed in the provided sources, but it is typically handled as a solid. For storage, it is recommended to keep the powder at low temperatures (e.g., -20°C) to maintain stability. These properties are important for its use in laboratory studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Pim1/AKK1-IN-1 are limited, as it is a research compound. Its primary value is as a tool for studying kinase signaling. While specific toxicity profiles are not detailed, its mechanism of inhibiting multiple kinases could potentially affect normal cellular processes, leading to off-target effects. However, comprehensive safety studies are not available in the public domain.
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| References | |
| Additional Infomation |
Pim1/AKK1-IN-1 is a research-use-only compound that acts as a potent multi-kinase inhibitor. It is also known as LKB1/AAK1 dual inhibitor and has the CAS number 1093222-27-5. This compound is used to study the roles of Pim1, AKK1, MST2, and LKB1 in various biological processes and diseases, particularly in cancer research. It is not an approved drug.
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| Molecular Formula |
C20H13N5O
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|---|---|
| Molecular Weight |
339.35012
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| Exact Mass |
339.112
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| CAS # |
1093222-27-5
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| Related CAS # |
1093222-27-5;
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| PubChem CID |
44588117
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| Appearance |
White to gray solid powder
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| Density |
1.42
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| LogP |
4.132
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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 |
550
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JTSLALYXYSRPGW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H13N5O/c21-9-13-3-5-14(6-4-13)16-8-17-18(12-24-19(17)23-11-16)25-20(26)15-2-1-7-22-10-15/h1-8,10-12H,(H,23,24)(H,25,26)
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| Chemical Name |
N-[5-(4-cyanophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyridine-3-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 : ~50 mg/mL (~147.34 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9468 mL | 14.7341 mL | 29.4681 mL | |
| 5 mM | 0.5894 mL | 2.9468 mL | 5.8936 mL | |
| 10 mM | 0.2947 mL | 1.4734 mL | 2.9468 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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