MPT0B392 |
Katalog-Nr.GC36652
One-Click Copy Product Info
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MPT0B392, ein oral aktives Chinolinderivat, induziert die Aktivierung der c-Jun-N-terminalen Kinase (JNK), was zu Apoptose fÜhrt. MPT0B392 hemmt die Tubulinpolymerisation und lÖst die Induktion des mitotischen Arrests aus, gefolgt von einem Verlust des mitochondrialen Membranpotentials und einer Caspasenspaltung durch Aktivierung von JNK und fÜhrt schließlich zur Apoptose. MPT0B392 erweist sich als neuartiges Mikrotubuli-depolymerisierendes Mittel und verstÄrkt die ZytotoxizitÄt von Sirolimus in Sirolimus-resistenten akuten LeukÄmiezellen und der mehrfach resistenten Zelllinie.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1346169-92-3
Sample solution is provided at 25 µL, 10mM.
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MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line[1]. JNK Caspase
MPT0B392 (B392) (0.001-0.1 μM; 24 and 48 hours) inhibits the cell viability of HL60, MOLT-4, and CCRF-CEM cells with IC50s of 0.02 μM, 0.03 μM and 0.02 μM, respectively[1].MPT0B392 (0.1 μM; 48 hours) induces apoptosis in HL60 cancer cells[1].MPT0B392 (0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours) triggers cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner[1].MPT0B392 (0.1 μM; 48 hours) increases the phosphorylation of Bcl-2, Mcl-1S and decreases in Mcl-1L[1]. Cell Viability Assay[1] Cell Line: HL60 (acute promyelocytic leukemia), MOLT-4 (acute lymphoblastic leukemia), CCRF-CEM (acute lymphoblastic leukemia) cells
The effects of MPT0B392 (oral gavage; 50 mg/kg or 100 mg/kg for 12 or 14 days) shows relative potent anti-leukemia activity in a vivo xenograft model[1]. Animal Model: Severe combined immunodeficient (SCID) mice [1]
[1]. Chao MW, et al. An oral quinoline derivative, MPT0B392, causes leukemic cells mitotic arrest and overcomes drug resistant cancer cells. Oncotarget. 2017 Apr,8(17):27772-27785.
| Cas No. | 1346169-92-3 | SDF | |
| Canonical SMILES | NC1=C2C(N=C(S(=O)(C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C2)=CC=C1OC | ||
| Formula | C19H20N2O6S | M.Wt | 404.44 |
| Löslichkeit | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4726 mL | 12.3628 mL | 24.7255 mL |
| 5 mM | 494.5 μL | 2.4726 mL | 4.9451 mL |
| 10 mM | 247.3 μL | 1.2363 mL | 2.4726 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)