| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Tubulin polymerization[1]
β-Tubulin (colchicine-binding site). MPT0B014 is a tubulin polymerization inhibitor that binds to the colchicine-binding site on β-tubulin, preventing microtubule assembly. This leads to G2/M cell cycle arrest and apoptosis. |
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| ln Vitro |
In a dosage-dependent way, MPT0B014 (0-1 μM; 48 h) suppresses the development of A549, H1299, and H226 cells [1]. A549 cells are exposed to MPT0B014 (0.05-0.3 μM) for 24 and 48 hours, which causes apoptosis by stopping the cell cycle in the G2/M and sub-G1 phases [1].
MPT0B014 inhibits proliferation of A549, H1299, and H226 human non-small cell lung cancer (NSCLC) cells with IC50s of 0.041, 0.046, and 0.041 µM, respectively. It also inhibits adriamycin-resistant NCI/ADR cells that overexpress P-glycoprotein with an IC50 of ~0.03 µM. |
| ln Vivo |
In vivo studies of rhininitib (0.75 and 1.0 mg/kg; sc once daily for 5 days till mice get moribund) demonstrate anti-AML effects[1
In vivo activity data for MPT0B014 is not extensively detailed in the literature. As a tubulin polymerization inhibitor, it is expected to show antitumor efficacy in animal models. Its potent activity against drug-resistant cells suggests it may overcome multidrug resistance. |
| Enzyme Assay |
In vitro tubulin polymerization assays are performed using purified tubulin protein and assessing the turbidity increase over time at 340 nm. The compound's ability to inhibit polymerization is measured, and IC50 values are calculated.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: A549, H1299, H226 and HUVEC cells Tested Concentrations: 0, 0.025, 0.05, 0.075 and 1 μM Incubation Duration: 48 h Experimental Results: Inhibited cell viability with IC50s of 0.109±0.01, 0.055±0.004, 0.077±0.005 and 0.536±0.166 μM against A549, H1299, H226 and HUVEC cells, respectively. Cell Cycle Analysis[1] Cell Types: A549, H1299 and H226 Tested Concentrations: 0.05, 0.1 and 0.3 μM Incubation Duration: 24 and 48 h Experimental Results: Treatment for 24 h led to notable accumulation of cells in the G2/M phase. At 48 h, sub-G1 apoptotic cell populations were increased in a concentration-dependent manner. Cells in the G2/M phase began to rise at 12 h post-treatment and peaked at 24 h. Following this, there was an emergence of cells in the sub-G1 population phase until 48 h. Western Blot Analysis[1] Cell Types: A549, H1299 and H226 Tested Concentrations: 0.05, 0.1 and 0.3 μM Incubation Duration: 24 h Experimental Results: Resulted in a marked increase in expression of the mitosis marker MPM2 and the proteins cyclin B1, Cdc2, Thr16 Cells (e.g., NSCLC cell lines) are treated with MPT0B014. Cell viability is measured using MTT or CellTiter-Glo assays. Cell cycle analysis is performed by flow cytometry. Apoptosis is assessed by Annexin V/PI staining and caspase activation. |
| Animal Protocol |
Animal/Disease Models: Nude athymic mice, A549 xenografts[1]
Doses: 100 mg/kg alone or in combination with 25 mg/kg Erlotinib (HY-50896) Route of Administration: iv/ip, daily for 25 days Experimental Results: The combined treatment resulted in more significant tumor growth delay (28%) compared with treatment alone (7%). The combination produced Dramatically higher anti-tumor activity. The growth of A549 cancer cell xenografts was suppressed by 11, 21 and 49% (tumor growth inhibition) after treatment with MPT0B014, Erlotinib and MPT0B014 plus Erlotinib, respectively. In vivo efficacy studies are performed in mouse xenograft models using NSCLC cells. MPT0B014 is administered intraperitoneally or intravenously. Tumor volume is measured by calipers. Tumors are harvested for histology and biomarker analysis. Body weight and clinical signs are monitored. |
| ADME/Pharmacokinetics |
MPT0B014 has a molecular weight of 323.34 and a molecular formula of C19H17NO4. It is a synthetic aroylquinoline derivative. It is soluble in DMSO. Detailed pharmacokinetic parameters such as oral bioavailability and half-life are available from specialized databases. It is stored at -20°C.
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| Toxicity/Toxicokinetics |
Detailed toxicological profiles of MPT0B014 are not extensively reported. As a tubulin inhibitor, it may cause dose-limiting toxicities such as myelosuppression and neurotoxicity, consistent with other agents in this class. Preclinical studies are needed to establish its safety profile.
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| References | |
| Additional Infomation |
MPT0B014 is a research-grade tubulin polymerization inhibitor. It is used in cancer research, particularly in studies of drug-resistant cancer cells. It is not approved for clinical use. Its molecular formula is C19H17NO4 and its molecular weight is 323.34.
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| Molecular Formula |
C19H17NO4
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|---|---|
| Molecular Weight |
323.34
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| Exact Mass |
323.115
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| Elemental Analysis |
C, 70.58; H, 5.30; N, 4.33; O, 19.79
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| CAS # |
1215208-59-5
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| Related CAS # |
1215208-59-5;
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| PubChem CID |
45139642
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
513.5±50.0 °C at 760 mmHg
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| Flash Point |
264.4±30.1 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.606
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| LogP |
3.17
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
416
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1=CC=C2C(=C1)C=CC=N2)(C1=CC(OC)=C(OC)C(OC)=C1)=O
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| InChi Key |
GSGXITQZCMSYKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17NO4/c1-22-16-10-14(11-17(23-2)19(16)24-3)18(21)13-6-7-15-12(9-13)5-4-8-20-15/h4-11H,1-3H3
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| Chemical Name |
quinolin-6-yl(3,4,5-trimethoxyphenyl)methanone
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| Synonyms |
MPT0B014; MPT0B-014; MPT0B 014; MPT 0B014; MPT-0B014; B014; B-014; B 014;
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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 mg/mL (154.64 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0927 mL | 15.4636 mL | 30.9272 mL | |
| 5 mM | 0.6185 mL | 3.0927 mL | 6.1854 mL | |
| 10 mM | 0.3093 mL | 1.5464 mL | 3.0927 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.
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