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Description: Dual Mer/Axl inhibitor
Chemical Name: 3-[4-[(Dimethylamino)methyl]phenyl]-N-methyl-N-[5-[3-methyl-5-(1,3,5-trimethyl-1H-pyrazol-4-yl)-2-pyridinyl]-1,3,4-oxadiazol-2-yl]imidazo[1,2-a]pyridine-6-methanamine
Purity: ≥97% (HPLC)
Biological Activity for AZ 14145845
AZ 14145845 is a potent, and highly selective dual Mer/Axl kinase inhibitor (pIC50 = 7 nM and 7.8 nM in pAxl and pMer, respectively). In vivo, AZ 14145845 shows dose-dependent reduction of tumor growth in the Mer and Axl kinase Ba/F3 tumor xenograft model. AZ 14145845 combined with anti-PD1 antibodies and ionizing radiation increases survival in mice with tumors derived from MC38 cells in vivo. AZ 14145845 is orally bioavailable.
Technical Data for AZ 14145845
| M. Wt | 561.69 |
| Formula | C32H35N9O |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 2830555-70-7 |
| PubChem ID | 156596359 |
| InChI Key | CZIXXCVLEHVEBZ-UHFFFAOYSA-N |
| Smiles | CC1=C(N=CC(C2=C(C)N(C)N=C2C)=C1)C3=NN=C(N(CC4=CN5C(C6=CC=C(CN(C)C)C=C6)=CN=C5C=C4)C)O3 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AZ 14145845
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 56.17 | 100 | |
| ethanol | 56.17 | 100 |
Preparing Stock Solutions for AZ 14145845
The following data is based on the product molecular weight 561.69. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.78 mL | 8.9 mL | 17.8 mL |
| 5 mM | 0.36 mL | 1.78 mL | 3.56 mL |
| 10 mM | 0.18 mL | 0.89 mL | 1.78 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Product Datasheets for AZ 14145845
References for AZ 14145845
References are publications that support the biological activity of the product.
McCoull et al (2021) Optimization of an Imidazo[1,2.a]pyridine series to afford highly selective type I1/2 Dual Mer/Axl kinase inhibitors with in vivo efficacy. J.Med.Chem. 64 13524 PMID: 34478292
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