| Size | Price | |
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| 1mg | ||
| Other Sizes |
| ln Vitro |
DLL4, JAG1/2 activity, and other Notch1 signals are inhibited by blintictuzumab (0-100 μg/mL)[1]. In the HPB-ALL cell line, blintictuzumab (25 μg/mL, 4 days) lowers the levels of Notch1 intracellular domain[1]. In MCL cells, blinitinib (25 μg/mL, 48 h) suppresses DLL4-mediated cleaved-Notch1 overexpression[2]. In Mino cells, brontictuzumab (25 μg/mL, 48 h) inhibits the enhanced phosphorylation of MEK and ERK caused by DLL4 stimulation[2].
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| ln Vivo |
In T-ALL xenografts, blintictuzumab (15 mg/kg, ip) decreases tumor burden[3]. In the MCL model, blintictuzumab (20 mg/kg, ip, every 4 days) suppresses DLL4-induced Notch1 activation[2].
|
| Cell Assay |
Western Blot Analysis[2]
Cell Types: DLL4 (4 μg/mL)-stimulated MCL cells Tested Concentrations: 25 μg/mL Incubation Duration: 24 or 48 h Experimental Results: Inhibited DLL4-dependent activation of Notch1. |
| Animal Protocol |
Animal/Disease Models: T-ALL xenograft[3]
Doses: 15 mg/kg Route of Administration: intraperitoneal (ip) injection (ip), twice weekly. Experimental Results: Inhibited tumor growth and decreased the size of the spleen. demonstrated massive infiltration and replacement of normal hematopoiesis by leukemia cells. Animal/Disease Models: NSG mice injected with DLL4-stimulated NOTCH1-mutated mino cells ex vivo[2] Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Inhibited cleaved Notch1 but was not enough to cause a significant efficacy in tumor growth. |
| References |
[1]. Ferrarotto R, et al. A phase I dose-escalation and dose-expansion study of brontictuzumab in subjects with selected solid tumors. Ann Oncol. 2018 Jul 1;29(7):1561-1568.
[2]. Silkenstedt E, et al. Notch1 signaling in NOTCH1-mutated mantle cell lymphoma depends on Delta-Like ligand 4 and is a potential target for specific antibody therapy. J Exp Clin Cancer Res. 2019 Nov 1;38(1):446. [3]. Agnusdei V, et al. Therapeutic antibody targeting of Notch1 in T-acute lymphoblastic leukemia xenografts. Leukemia. 2014 Feb;28(2):278-88. |
| CAS # |
1447814-75-6
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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.) |
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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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