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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.82%
- 分子式: C27H25F6N5O7
- 分子量:645.51
-
保管条件:
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]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Breast Cancer Compound Library
HY-L074
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cytokine Inhibitors Library
HY-L161
-
Macrophage Related Compound Library
HY-L174
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
生物活性
|
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.
化学情報
-
性状 Solid
-
分子量 645.51
-
分子式 C27H25F6N5O7
-
Color Off-white to light yellow
-
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
-
別名
Q702 TFA
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (273 KB)
-
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)
-
取扱説明書 (2659 KB)
参考文献
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 |
|---|---|---|---|---|---|
| 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 関連分類
HY-152830A 関連分類
Powered by Bioz