| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
AZ82 targets KIFC1 (HSET), a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes. It is a selective inhibitor of KIFC1 with a Ki of 43 nM and an IC₅₀ of 300 nM. AZ82 binds to the KIFC1/microtubule complex but not to KIFC1 or microtubules alone. It disrupts mitotic spindle formation by inhibiting kinesin motor activity, thereby blocking cell division.
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| ln Vitro |
AZ82 lightning-induced multipolar spindles in BT-549 cells, but not in IR with normal centrosome counts, such as HeLa [1]. AZ82 binds to the KIFC1/MT complex but not to KIFC1 or MT alone. Treatment with AZ82 resulted in centrosome declustering and centrosome amplification in BT-549 breast cancer cells. The IC50 of AZ82 that inhibits mant-ATP binding is 0.90 ± 0.09 μM, whereas the IC50 that releases mant-ADP is 1.26 ± 0.51μM[2].
In vitro, AZ82 induces multipolar spindles in BT-549 breast cancer cells (which have supernumerary centrosomes) but not in cells with normal centrosome counts such as HeLa. Treatment with AZ82 results in centrosome declustering and centrosome amplification in BT-549 cells. The IC₅₀ of AZ82 that inhibits mant-ATP binding is 0.90 ± 0.09 μM, whereas the IC₅₀ that releases mant-ADP is 1.26 ± 0.51 μM. |
| ln Vivo |
In vivo activity of AZ82 has not been extensively characterized in animal models. The compound is primarily used as a research tool for in vitro studies of KIFC1 function and mitotic spindle organization. Its potential as an anticancer agent requires further evaluation in vivo. Currently, no specific in vivo data are available in the published literature.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for AZ82 typically involve studying its binding to KIFC1 and microtubules. The compound is incubated with purified KIFC1 protein and microtubules in appropriate buffer. Binding affinity is assessed using surface plasmon resonance (SPR) or fluorescence-based assays. The compound's ability to inhibit mant-ATP binding and mant-ADP release is measured to determine IC₅₀ values.
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| Cell Assay |
In vitro cell-based assays for AZ82 typically employ cancer cell lines with supernumerary centrosomes such as BT-549 breast cancer cells. Cells are cultured and treated with various concentrations of the compound. Endpoints include assessment of spindle morphology by immunofluorescence microscopy, centrosome clustering analysis, cell cycle analysis by flow cytometry, and cell viability assessment by MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal studies with AZ82 have not been extensively reported. The compound is a research tool for in vitro studies. Future studies may involve administration of the compound in rodent xenograft models of cancer to evaluate its antitumor efficacy. Currently, no specific in vivo data are available.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of AZ82 have not been characterized. As a small molecule with a molecular weight of 560.63, the compound may have reasonable cell permeability and oral bioavailability. However, specific PK parameters have not been determined. The compound is soluble in DMSO and should be stored at -20°C.
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| Toxicity/Toxicokinetics |
The toxicity profile of AZ82 has not been characterized in preclinical studies. The compound is intended for research use only and is not approved for human therapeutic applications. No specific toxicology data are available. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
AZ82 is a research-grade selective KIFC1 inhibitor used in cancer research to study mitotic spindle formation and centrosome clustering. It is not an approved therapeutic drug and has no clinical trial history. The compound is supplied as a white to off-white solid powder with purity ≥98% and should be stored at -20°C. Synonyms include 5-methyl-N-[(2R)-1-oxo-1-[[(3R)-pyrrolidin-3-yl]amino]-3-[6-[3-(trifluoromethoxy)phenyl]pyridin-3-yl]propan-2-yl]-4-propylthiophene-2-carboxamide.
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| Molecular Formula |
C28H31F3N4O3S
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|---|---|
| Molecular Weight |
560.630955934525
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| Exact Mass |
560.206
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| CAS # |
1449578-65-7
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| PubChem CID |
91885438
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| Appearance |
White to off-white solid powder
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| LogP |
5.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
39
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| Complexity |
819
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S1C(C)=C(CCC)C=C1C(N[C@H](CC1C=NC(C2C=CC=C(C=2)OC(F)(F)F)=CC=1)C(N[C@H]1CNCC1)=O)=O
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| InChi Key |
PMTLKNOARSHUJB-ZJSXRUAMSA-N
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| InChi Code |
InChI=1S/C28H31F3N4O3S/c1-3-5-19-14-25(39-17(19)2)27(37)35-24(26(36)34-21-10-11-32-16-21)12-18-8-9-23(33-15-18)20-6-4-7-22(13-20)38-28(29,30)31/h4,6-9,13-15,21,24,32H,3,5,10-12,16H2,1-2H3,(H,34,36)(H,35,37)/t21-,24-/m1/s1
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| Chemical Name |
5-methyl-N-[(2R)-1-oxo-1-[[(3R)-pyrrolidin-3-yl]amino]-3-[6-[3-(trifluoromethoxy)phenyl]pyridin-3-yl]propan-2-yl]-4-propylthiophene-2-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 : ~125 mg/mL (~222.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.71 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 (3.71 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 20.8 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 | 1.7837 mL | 8.9185 mL | 17.8371 mL | |
| 5 mM | 0.3567 mL | 1.7837 mL | 3.5674 mL | |
| 10 mM | 0.1784 mL | 0.8919 mL | 1.7837 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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