| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
AXL, GAS6[1][2].
Growth arrest-specific protein 6 (GAS6). Batiraxcept binds to GAS6, the only known ligand for the AXL receptor. By doing so, it prevents GAS6 from activating AXL, thereby blocking AXL-mediated signaling pathways involved in tumor progression, metastasis, and immune evasion. |
|---|---|
| ln Vitro |
Batiraxcept binds to human GAS6 with high affinity, substantially reducing AXL-signaled invasion and migration of highly metastatic cells in vitro. As a protein therapeutic, it does not have an IC50 in the traditional sense but acts as a ligand trap, showing potent biological activity at low nanomolar concentrations.
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| ln Vivo |
In nonclinical models of aggressive human cancers, batiraxcept treatment leads to significant inhibition of metastatic disease. In patient-derived xenograft models, it has been shown to inhibit the growth and metastasis of various tumors, including prostate cancer, and improve responses to chemotherapy and immunotherapy.
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| Enzyme Assay |
Cell-free GAS6 binding assays are performed using surface plasmon resonance or ELISA. Recombinant human GAS6 is immobilized on a sensor chip or plate, and increasing concentrations of batiraxcept are flowed over. Binding affinity is determined from the association and dissociation rates. Alternatively, competition assays with labeled AXL-Fc can be performed.
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| Cell Assay |
Human cancer cell lines expressing high levels of AXL are cultured in 3D matrices or transwell chambers. Cells are treated with batiraxcept and stimulated with GAS6. Inhibition of invasion and migration is quantified by counting cells that invade through the membrane. The effect on downstream signaling (e.g., pAKT, pERK) is assessed by Western blot.
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| Animal Protocol |
For in vivo studies, batiraxcept is administered to mice via intraperitoneal (IP) injection. In metastasis models, it is given weekly or bi-weekly. Tumor growth and metastasis are monitored by bioluminescence imaging or histology. In combination studies, it is administered alongside chemotherapy or immune checkpoint inhibitors.
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| ADME/Pharmacokinetics |
Dosing: 15 mg/kg intraperitoneally (i.p.) weekly. The elimination half-life of batiraxcept in humans is approximately 15 days. As a large 129 kDa fusion protein, it has a low volume of distribution (3-5 L). Clearance is typical of a monoclonal antibody, and it does not cross the blood-brain barrier.
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| Toxicity/Toxicokinetics |
No specific toxicity data are detailed, but as an AXL inhibitor, the primary risk is based on target-mediated effects. In preclinical studies, batiraxcept was well-tolerated. Clinical trial data indicate a manageable safety profile with mild to moderate adverse events, primarily gastrointestinal and fatigue. No dose-limiting toxicities were observed.
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| References |
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| Additional Infomation |
Other information: Batiraxcept has been granted Fast Track designation by the FDA. It has completed Phase 1b/2 clinical trials in combination with durvalumab for ovarian cancer and with paclitaxel for ovarian and pancreatic cancer. It is a first-in-class GAS6-AXL inhibitor that is not orally active. Its CAS number is 2268717-61-7.
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| CAS # |
2268717-61-7
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|---|---|
| Appearance |
Colorless to light yellow liquid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| 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.) |
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.
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