| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| References | |
|---|---|
| Additional Infomation |
Adrixetinib is a small molecule drug. The International Nonproprietary Name (INN) prefix "-tinib" in its name indicates that adrixetinib is a tyrosine kinase inhibitor. The monoisotope molecular weight of adrixetinib is 531.17 Da. Adrixetinib is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor that inhibits Axl (UFO), Mer, and colony-stimulating factor-1 receptors (CSF1R; CSF-1R; CD115; M-CSFR), possessing potential immunomodulatory, chemosensitizing, and antitumor activities. After oral administration, adrixetinib targets and blocks the activity of Axl, Mer, and CSF1R, thereby blocking Axl, Mer, and CSF1R-mediated signaling pathways. This inhibits the proliferation of tumor cells expressing Axl and Mer. Furthermore, blocking Axl and Mer-mediated signaling pathways may reactivate the innate immune system against cancer cells. Blocking the CSF1R-mediated signaling pathway inhibits the activity of tumor-associated macrophages (TAMs), regulatory T cells (Tregs), and the recruitment of myeloid-derived suppressor cells (MDSCs). In summary, this can eliminate immunosuppression in the tumor microenvironment (TME), enhance anti-tumor T cell immune responses, and inhibit tumor cell proliferation. CSF1R, also known as macrophage colony-stimulating factor receptor (M-CSFR) and CD115 (differentiation cluster 115), is a cell surface receptor that plays a crucial role in tumor cell proliferation, metastasis, and cancer-related immunosuppression. Axl and Mer are both members of the TAM (Tyro3, Axl, and Mer) family of RTKs and are overexpressed in various tumor cell types. They play key roles in tumor cell proliferation, survival, invasion, angiogenesis, metastasis, and inactivation of innate immunity in cancer. Their expression is associated with drug resistance and poor prognosis.
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| Molecular Formula |
C25H24F3N5O5
|
|---|---|
| Molecular Weight |
531.483776092529
|
| Exact Mass |
531.172
|
| CAS # |
2394874-66-7
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| Related CAS # |
Adrixetinib TFA
|
| PubChem CID |
156440741
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.3
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
38
|
| Complexity |
765
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N1(CCC)C=C(OCC(F)(F)F)C(C(NC2=NC=C(OC3C4C(N=CC=3)=CC(OC)=C(OC)C=4)C=C2)=O)=N1
|
| InChi Key |
BWUUJXXFCSYLFW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C25H24F3N5O5/c1-4-9-33-13-21(37-14-25(26,27)28)23(32-33)24(34)31-22-6-5-15(12-30-22)38-18-7-8-29-17-11-20(36-3)19(35-2)10-16(17)18/h5-8,10-13H,4,9,14H2,1-3H3,(H,30,31,34)
|
| Chemical Name |
N-[5-(6,7-dimethoxyquinolin-4-yl)oxypyridin-2-yl]-1-propyl-4-(2,2,2-trifluoroethoxy)pyrazole-3-carboxamide
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| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ≥ 100 mg/mL (188.15 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8815 mL | 9.4077 mL | 18.8154 mL | |
| 5 mM | 0.3763 mL | 1.8815 mL | 3.7631 mL | |
| 10 mM | 0.1882 mL | 0.9408 mL | 1.8815 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT07138196
Conditions:Chronic Graft-Versus-Host DiseaseProducts are for research use only; We do not sell to patients
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