2394874-66-7
2394874-66-7
Chemical Structure
Adrixetinib
Synonym(s): Q702
- CAS No.: 2394874-66-7
- Formula:C25H24F3N5O5
- Molecular Weight:531.48
IUPAC Name: (S)-2-hydroxy-6-((4-(2-(2-hydroxyethyl)nicotinoyl)morpholin-3-yl)methoxy)benzaldehyde
InChIKey: BWUUJXXFCSYLFW-UHFFFAOYSA-N
SMILES: O=C(C1=NN(CCC)C=C1OCC(F)(F)F)NC2=NC=C(C=C2)OC3=C4C=C(OC)C(OC)=CC4=NC=C3
Biological Activity: Adrixetinib (Q702) is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Adrixetinib | 99.55% | Adrixetinib (Q702) is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma. | ||||||||||||||||||||
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Ki8751 | 99.76% | Ki8751 is a potent VEGFR2 inhibitor with an IC50 of 0.9 nM. | ||||||||||||||||||||
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LDC1267 | 99.64% | LDC1267 is a AXL/TAM/FLT3 inhibitor with IC50 values of 42 nM, 130 nM, and 63 nM against AXL, MERTK, and TYRO3, respectively. LDC1267 blocks GAS6-induced AXL phosphorylation and the downstream AKT/ERK1/2 signaling pathway. LDC1267 inhibits cancer cell proliferation, colony formation, and glioblastoma cell invasion, without causing obvious impairment of cytotoxic autophagic flux. LDC1267 exerts a synergistic effect when used in combination with Imatinib (HY-15463) in chronic myeloid leukemia models. LDC1267 can be widely applied in studies related to glioblastoma and chronic myeloid leukemia. | ||||||||||||||||||||
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AMG-458 | 98.41% | AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively. | ||||||||||||||||||||
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JNK2-IN-1 | JNK2-IN-1 (Compound J27) is a JNK2 inhibitor (Kds: 79.2 μM). JNK2-IN-1 has anti-inflammatory activity. JNK2-IN-1 decreases the release of TNF-α and IL-6 through inhibiting the activation of NF-κB/MAPK pathway. JNK2-IN-1 alleviates the symptoms of LPS-induced acute lung injury (ALI) and sepsis. | |||||||||||||||||||||
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Axl/Mer/CSF1R-IN-1 | Axl/Mer-IN-1 (Compound 1) is an Axl/Mer receptor tyrosine kinase (Axl/Mer RTK) and CSF1R inhibitor with Kds of <0.1 μM. | |||||||||||||||||||||
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Axl/Mer/CSF1R-IN-2 | Axl/Mer/CSF1R-IN-2 (Comp 4) is a Axl, Mer and CSF1R inhibitor. | |||||||||||||||||||||
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Lucitanib dihydrochloride | 98.12% | Lucitanib (E-3810) dihydrochloride is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. | ||||||||||||||||||||
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KIN-8741 | KIN-8741 is a highly selective Type IIb c-Met inhibitor. KIN-8741 has broad activity against c-Met kinase mutations. KIN-8741 shows antitumor activity in MET gene amplified and exon 14 deleted non-small cell lung cancer models. KIN-8741 can be used in the research of c-Met driven cancers, especially advanced tumors carrying MET exon 14 jump mutations, acquired drug resistance mutations, etc. | |||||||||||||||||||||
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AZD2932 | 98.16% | AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively. | ||||||||||||||||||||
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K812 | K812 is an orally active ASK1 inhibitor with a 6 nM IC50 against ASK1. K812 selectively inhibits ASK1 activation. K812 inhibits glial activation in the lumbar spinal cord. K812 extends survival of SOD1G93A transgenic mice. K812 can be used for the research of amyotrophic lateral sclerosis. | |||||||||||||||||||||
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References
- [1]. Jeon Y, et al. A Novel Selective Axl/Mer/CSF1R Kinase Inhibitor as a Cancer Immunotherapeutic Agent Targeting Both Immune and Tumor Cells in the Tumor Microenvironment. Cancers (Basel). 2022;14(19):4821. Published 2022 Oct 2. [Content Brief]
- [2]. NAM K, et al. Quinoline derivatives as inhibitors of axl/mer rtk and csf1r. WO, WO2019229251A1, 2019-12-05.
