| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
MBM-55 (42g compound) has IC50s of 0.53, 0.84, and 7.13 μM, respectively, which inhibit the growth of MGC-803, HCT-116, and Bel-7402 cells [1]. In HCT-116 cells, MBM-55 (0.5-1 μM; 24 hours) stimulates cell engraftment in a concentration-evaporative manner [1]. causes the G2/M phase arrest and the build-up of cells in 116 cells that contain more than 4N [1].
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|---|---|
| ln Vivo |
In nude mice with HCT-116 xenografts, MBM-55 (20 mg/kg; i.p.; twice daily for 21 days) showed strong anti-activity and a well-tolerated dosing schedule [1]. CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, and 495 ng/h were observed after MBM-55 (1.0 mg/kg; IV) therapy, respectively.
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| Cell Assay |
Cell cycle analysis [1]
Cell Types: HCT-116 cells Tested Concentrations: 0.5, 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: Cells that induce G2/M phase arrest and accumulate >4N content. Apoptosis analysis [1] Cell Types: HCT-116 Cell Tested Concentrations: 0.5, 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: Cell apoptosis was induced in a concentration-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Female BALB/c nu/nu (nude) mice (5-6 weeks, bearing HCT-116 xenograft) [1]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection; /mL and 507 ng/h/ mL. Twice a day for 21 days Experimental Results: Significant inhibition of tumor growth. Animal/Disease Models: Male SD rat[1] Doses: 1.0 mg/kg Route of Administration: intravenous (iv) (iv)injection (pharmacokinetic/PK/PK analysis) Experimental Results: CL, Vss, T1/2, AUC0-t, AUC0-∞ values are 33.3 mL /min/kg, 2.53 L/kg, 1.72 h, 495 ng/h/mL and 507 ng/h/mL respectively. |
| References |
| Molecular Formula |
C28H27FN6O2
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|---|---|
| Molecular Weight |
498.551388978958
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| Exact Mass |
498.217
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| CAS # |
2083622-09-5
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| Related CAS # |
MBM-55S;2083624-07-9
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| PubChem CID |
137636872
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| Appearance |
White to off-white solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
37
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| Complexity |
758
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC=CC(=C1)COC1=C(C(N)=O)C=CC(=C1)C1=CN=C2C=C(C=CN12)C1C=NN(C=1)CCN(C)C
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| InChi Key |
CGECJCJUHCZZGO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H27FN6O2/c1-33(2)10-11-34-17-22(15-32-34)20-8-9-35-25(16-31-27(35)14-20)21-6-7-24(28(30)36)26(13-21)37-18-19-4-3-5-23(29)12-19/h3-9,12-17H,10-11,18H2,1-2H3,(H2,30,36)
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| Chemical Name |
4-[7-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]-2-[(3-fluorophenyl)methoxy]benzamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~125 mg/mL (~250.73 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 | 2.0058 mL | 10.0291 mL | 20.0582 mL | |
| 5 mM | 0.4012 mL | 2.0058 mL | 4.0116 mL | |
| 10 mM | 0.2006 mL | 1.0029 mL | 2.0058 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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