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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| ln Vitro |
Xaluritamig (AMG-509) specifically binds to 293T cells transfected with human STEAP1, with an EC50 of 3.8 nM[2]. Xaluritamig effectively induces T cell-mediated lysis of STEAP1-positive human cancer cells, with a median EC50 of 37 pM in 19 cell lines; it has no activity against STEAP1 knockout prostate cancer cells[2]. Xaluritamig is more effective than anti-STEAP1 Fab XmAb molecules in inducing prostate cancer cell lysis; it preferentially kills cancer cells with high STEAP1 expression and has very low activity against normal cells[2]. Xaluritamig induces only very low levels of cytotoxicity in cultured human normal bronchial smooth muscle cells and aortic endothelial cells with low STEAP1 expression[3].
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| ln Vivo |
Xaluritamig (0.01–1 mg/kg; intravenous injection; twice administered at 7-day intervals; total treatment duration 16 days) showed significant antitumor activity in the subcutaneous 22Rv1-LucSTEAP1 xenograft model in NSG mice, with a tumor growth inhibition rate of 99.7% (complete cessation of tumor growth) in the 0.01 mg/kg dose group [4]. Xaluritamig (0.3 mg/kg; intravenous injection; twice administered at 7-day intervals; total treatment duration 17 days) significantly inhibited tumor growth in the Myc-CaP-LucSTEAP1 tibial bone metastasis model in FVB/N huCD3ε knock-in mice, but its antitumor activity was not enhanced when combined with anti-PD-1 antibody [4]. Xaluritamig (10 μg/kg, or an additional 40 μg/kg; intravenous injection; for 28 consecutive days) was well tolerated in male and female Mauritian cynomolgus monkeys. Serum exposure was almost dose-proportional and there was no serious target-related off-target toxicity [4].
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| Animal Protocol |
Animal/Disease Models:Male NSG mice (NOD.Cg-Prkdcscid Il2rgtm1N/j/SzJ), weight and age not specified + 22Rv1-LucSTEAP1 subcutaneous xenograft model [4]
Doses: 0.01 mg/kg, 0.1 mg/kg, 1 mg/kg Route of Administration: Intravenous injection; twice, 7 days apart; for 16 days. Experimental Results: Significant antitumor activity was observed. In the 0.01 mg/kg dose group, after administration twice on days 9 and 16, the tumor growth inhibition rate reached 99.7%, and the tumor completely stopped growing; in the 0.1 mg/kg and 1 mg/kg dose groups, after administration twice on days 9 and 16, the tumor regression rates were 61.6% and 66.2%, respectively. Animal/Disease Models:Male and female cynomolgus monkeys (Mauritius), normal toxicology assessment model [4] Doses: 10 μg/kg fixed dose, 10 μg/kg initial dose, followed by 40 μg/kg weekly. Route of Administration: Intravenous injection; single dose group: once; escalation dose group: four times; 28 days. Experimental Results: During the 28-day study, subjects tolerated the study well, serum exposure was nearly proportional to dose, and there were no sex differences. Transient changes associated with acute phase response were observed, including increased C-reactive protein, decreased absolute counts of total T cells, cytotoxic T cells, helper T cells and natural killer cells, and mild increases in neutrophils and globulins. No serious target-related off-target toxicity was detected. |
| References |
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| Molecular Formula |
PLEASEREFERTOTHELOT-SPECIFICCOAFORSPECIFICBUFFERINFORMA
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|---|---|
| Molecular Weight |
173.555 kDa
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| CAS # |
2559056-68-5
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| Related CAS # |
Cell-ATP Viability Detection Kit; Protein A Agarose; HOLO Human Interleukin-2 (IL-2) Detection Kit; Bradford Protein Assay Kit; Cell Counting Kit-8
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| Appearance |
Colorless to light yellow liquid
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| Synonyms |
AMG-509
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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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