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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Bozitinib (Vebreltinib; formerly APL-101/PLB-1001, CBT-101) is a novel, an ATP-competitive, and highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) attaches itself to the tyrosine kinase superfamily's typical ATP-binding pocket. Phase I/II trials are presently investigating it as a single agent in patients with solid tumors, non-small cell lung cancer (NSCLC), and glioblastomas; additionally, it is being investigated in patients with hepatocellular carcinoma and renal cell carcinoma in combination with PD-L1 inhibitors. Due to its ability to cross the blood–brain barrier, the medication has shown promise in treating glioblastoma and has shown anticancer effects in a number of human xenograft tumor models with MET dysregulation. A small number of patients with chemotherapy-resistant, MET-altered gliomas have shown the drug's safety and preliminary efficacy. In China, a phase II trial (NCT04258033) is assessing bozitinib in patients with non-small cell lung cancer (NSCLC) who have skipped MET exon 14.
Targets |
c-Met
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ln Vitro |
The phosphorylation of MET and STAT3 is inhibited by bozitinib (PLB-1001) (30 μM; 6 hours), and PLB-1001 has more inhibitory effects on MET and its downstream signaling buffers.
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Cell Assay |
Western Blot analysis [1]
Cell Types: human astrocytes (HA) Cell Tested Concentrations: 30 μM Incubation Duration: 6 hrs (hours) Experimental Results: p-STAT3, p-MET expression diminished. |
References |
[1]. Hu H, et al. Mutational Landscape of Secondary Glioblastoma Guides MET-Targeted Trial in Brain Tumor. Cell. 2018 Nov 29;175(6):1665-1678.e18.
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Molecular Formula |
C₂₀H₁₅F₃N₈
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Molecular Weight |
424.381912469864
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Exact Mass |
424.14
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Elemental Analysis |
C, 56.60; H, 3.56; F, 13.43; N, 26.40
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CAS # |
1440964-89-5
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Related CAS # |
1440964-89-5
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Appearance |
Solid powder
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SMILES |
CN1C=C2C=C(C(=CC2=N1)F)C(C3=NN=C4N3N=C(C=C4)C5=CN(N=C5)C6CC6)(F)F
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InChi Key |
QHXLXUIZUCJRKV-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H15F3N8/c1-29-9-11-6-14(15(21)7-17(11)27-29)20(22,23)19-26-25-18-5-4-16(28-31(18)19)12-8-24-30(10-12)13-2-3-13/h4-10,13H,2-3H2,1H3
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Chemical Name |
6-(1-cyclopropylpyrazol-4-yl)-3-[difluoro-(6-fluoro-2-methylindazol-5-yl)methyl]-[1,2,4]triazolo[4,3-b]pyridazine
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Synonyms |
PLB 1001; Bozitinib; PLB-1001; PLB1001; CBT101; CBT 101; CBT-101; Vebreltinib
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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) |
DMSO: 50~85 mg/mL (200.3~117.8 mM)
Ethanol: ~2.5 mg/mL (~5.9 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3564 mL | 11.7819 mL | 23.5638 mL | |
5 mM | 0.4713 mL | 2.3564 mL | 4.7128 mL | |
10 mM | 0.2356 mL | 1.1782 mL | 2.3564 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.