| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
It was investigated how URMC-099 (URMC099) affected the in vitro proliferation of "brain-homing" MDA-MB-231 BR cells that expressed eGFP (eGFP8.4) and the cell line that gave rise to them. Both the vehicle and 200 nM URMC-099 were used to treat the cells. The growth rate of cells treated with URMC-099 was comparable to that of cells treated with vehicle. All cases had cell viability greater than 99% [2].
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| ln Vivo |
The terminal elimination half-life of URMC-099 is intermediate for C57 BL/6 mice (10 mg/kg, p.o. ), mg/kg, iv), and C57 BL/6 mice (10 mg/kg, iv) with t1/2=1.92 h, 2.14 h, and 2.72 h[1]. URMC-099 (URMC099) was examined for its impact on tumor formation in vivo by means of a well-established mice xenograft model of brain metastasis from breast cancer. Immunodeficient nu/nu mice were used in these studies, and after injecting eGFP8.4 cells into their left ventricle, the animals were given either vehicle or URMC-099 (10 mg/kg) every 12 hours for 20 days. Because it has been demonstrated to be sufficient to inhibit MLK3 in mice, has strong penetration of the blood-brain barrier, and efficiently suppresses the phosphorylation of Jun N-terminal kinase (JNK) in brain tissue, this dosage of URMC-099 was selected. Mice were slaughtered on day 21 and the BM number was determined. Each treatment group included of fifteen mice. 60% of the animals had BM, which is in line with other researchers' earlier investigations utilizing this xenograft model. The total number of brain metastases (BM) in mice was significantly (p<0.05, two-tailed t-test) increased by URMC-099 therapy. The pattern for micrometastases was comparable to the overall BM pattern. The number of macrometastases in mice treated with vehicle or URMC-099 was not significantly different [2].
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| References |
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| Molecular Formula |
C27H27N5
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|---|---|
| Molecular Weight |
421.5368
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| Exact Mass |
421.226
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| CAS # |
1229582-33-5
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| PubChem CID |
54764565
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.711
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| LogP |
3.85
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
611
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QKKIWEILHCXECO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H27N5/c1-31-10-12-32(13-11-31)18-19-2-4-20(5-3-19)23-15-24-25(17-30-27(24)29-16-23)21-6-7-26-22(14-21)8-9-28-26/h2-9,14-17,28H,10-13,18H2,1H3,(H,29,30)
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| Chemical Name |
3-(1H-indol-5-yl)-5-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine
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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 : ≥ 33 mg/mL (~78.28 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.87 mg/mL (6.81 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.87 mg/mL (6.81 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 (4.93 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. Solubility in Formulation 4: ≥ 2.08 mg/mL (4.93 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. Solubility in Formulation 5: ≥ 2.08 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3723 mL | 11.8613 mL | 23.7225 mL | |
| 5 mM | 0.4745 mL | 2.3723 mL | 4.7445 mL | |
| 10 mM | 0.2372 mL | 1.1861 mL | 2.3723 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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