2830555-70-7
Chemical Structure
AZ14145845
- CAS No.: 2830555-70-7
- Formula:C32H35N9O
- Molecular Weight:561.68
IUPAC Name: N-((3-(4-((dimethylamino)methyl)phenyl)imidazo[1,2-a]pyridin-6-yl)methyl)-N-methyl-5-(3-methyl-5-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridin-2-yl)-1,3,4-oxadiazol-2-amine
InChIKey: CZIXXCVLEHVEBZ-UHFFFAOYSA-N
SMILES: CC1=C(C2=CN=C(C3=NN=C(N(CC4=CN5C(C=C4)=NC=C5C6=CC=C(CN(C)C)C=C6)C)O3)C(C)=C2)C(C)=NN1C
Biological Activity: AZ14145845 is an orally active dual-target type 1½ kinase inhibitor of Mer/Axl, which inhibits Mer kinase (pIC50 = 9.0) and Axl kinase (pIC50 = 7.9) with high selectivity over Flt3 and Tyro3. AZ14145845 suppresses Mer- and Axl-dependent proliferation in Ba/F3 cells and inhibits efferocytosis in macrophages. AZ14145845 reduces the phagocytosis of photoreceptor outer segments by polarized human retinal epithelial cells. AZ14145845 inhibits tumor growth and induces tumor regression in vivo, and its combination with anti-PD1 antibody and ionizing radiation improves the survival rate of mice with colorectal cancer. AZ14145845 causes retinal degeneration in mice, with pathological changes similar to those in MERTK loss-of-function models. AZ14145845 can be used in studies related to retinal degeneration, lymphoma and colorectal cancer[1][2].
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AZ14145845 | 98.00% | AZ14145845 is an orally active dual-target type 1½ kinase inhibitor of Mer/Axl, which inhibits Mer kinase (pIC50 = 9.0) and Axl kinase (pIC50 = 7.9) with high selectivity over Flt3 and Tyro3. AZ14145845 suppresses Mer- and Axl-dependent proliferation in Ba/F3 cells and inhibits efferocytosis in macrophages. AZ14145845 reduces the phagocytosis of photoreceptor outer segments by polarized human retinal epithelial cells. AZ14145845 inhibits tumor growth and induces tumor regression in vivo, and its combination with anti-PD1 antibody and ionizing radiation improves the survival rate of mice with colorectal cancer. AZ14145845 causes retinal degeneration in mice, with pathological changes similar to those in MERTK loss-of-function models. AZ14145845 can be used in studies related to retinal degeneration, lymphoma and colorectal cancer. | ||||||||||||||||||||
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References
- [1]. Hamm G, et al. Pharmacological inhibition of MERTK induces in vivo retinal degeneration: a multimodal imaging ocular safety assessment. Arch Toxicol. 2022;96(2):613-624.
- [2]. McCoull W, et al. 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. 2021 Sep 23;64(18):13524-13539. [Content Brief]
