Adrixetinib TFA
Based on 1 Customer Validation
Adrixetinib (Q702) TFA 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 TFA acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib TFA increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib TFA upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib TFA shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib TFA is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.82%
- Formel: C27H25F6N5O7
- Molecular Weight:645.51
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Help & FAQs
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Biologische Aktivität
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Axl 0.3 nM (Kd) |
Mer 0.8 nM (Kd) |
MHC I |
Adrixetinib (Q702; 1 h) TFA potently binds to and inhibits purified Axl, Mer, and CSF1R kinases with IC50 values of 0.3 nM, 0.8 nM, and 8.7 nM, respectively[1].
Adrixetinib (0.001-10 μM; 24 h pretreatment) TFA concentration-dependently inhibits Gas6-induced phosphorylation of Axl and AKT in H1299 cells, concentration-dependently inhibits Gas6-induced phosphorylation of Mer and AKT in A549 cells, and concentration-dependently inhibits CSF1-induced phosphorylation of CSF1R and ERK in THP-1 cells[1].
Adrixetinib (0.1-100 μM; 72 h) TFA directly inhibits EMT6 cell viability with an IC50 of 8.4 μM[1].
Adrixetinib TFA inhibits M-NFS-60 cell proliferation through the CSF1R pathway with an IC50 < 1.0 μM, showing potent cellular activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Adrixetinib (10-100 mg/kg; p.o.; daily; 14 days) TFA induces dose-dependent tumor growth control (54.3% to 84.6%) in subcutaneous EMT6 syngeneic breast cancer tumors in BALB/c mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; up to 7 days) TFA modulates EMT6 gene expression in subcutaneous EMT6 tumors to promote an immune-stimulatory microenvironment in BALB/c mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; 5 to 22 days) TFA remodels the immune cell population in subcutaneous MHC-I and E-cadherin expression in BALB/c mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; 7 days) TFA enhances the effector function of T and natural killer cells by increasing IFN-γ and granzyme B production in both subcutaneous EMT6 tumors and peripheral blood of BALB/c mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; 21 days) TFA increases CD8 T cell infiltration, reduces myeloid cell accumulation, and upregulates MHC-I and PD-L1 expression in subcutaneous EMT6 tumors in BALB/c mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; 9 days) TFA increases tumor antigen-specific CD8 T cell infiltration into subcutaneous B16F10-OVA melanoma tumors in C57BL/6 mice[1].
Adrixetinib (30 mg/kg; p.o.; daily; up to 27 days) TFA induces tumor growth inhibition (64% to 77% TGI) in subcutaneous CT26, MC38, and RENCA syngeneic tumor models in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 645.51
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Formel C27H25F6N5O7
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Color Off-white to light yellow
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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.OC(C(F)(F)F)=O
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Synonyms
Q702 TFA
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (154.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.5492 mL | 7.7458 mL | 15.4916 mL | 38.7291 mL |
| 5 mM | 0.3098 mL | 1.5492 mL | 3.0983 mL | 7.7458 mL | |
| 10 mM | 0.1549 mL | 0.7746 mL | 1.5492 mL | 3.8729 mL | |
| 15 mM | 0.1033 mL | 0.5164 mL | 1.0328 mL | 2.5819 mL | |
| 20 mM | 0.0775 mL | 0.3873 mL | 0.7746 mL | 1.9365 mL | |
| 25 mM | 0.0620 mL | 0.3098 mL | 0.6197 mL | 1.5492 mL | |
| 30 mM | 0.0516 mL | 0.2582 mL | 0.5164 mL | 1.2910 mL | |
| 40 mM | 0.0387 mL | 0.1936 mL | 0.3873 mL | 0.9682 mL | |
| 50 mM | 0.0310 mL | 0.1549 mL | 0.3098 mL | 0.7746 mL | |
| 60 mM | 0.0258 mL | 0.1291 mL | 0.2582 mL | 0.6455 mL | |
| 80 mM | 0.0194 mL | 0.0968 mL | 0.1936 mL | 0.4841 mL | |
| 100 mM | 0.0155 mL | 0.0775 mL | 0.1549 mL | 0.3873 mL |
Adrixetinib TFA Related Classifications
HY-152830A Related Classifications
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