| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Verubulin hydrochloride (MPC-6827 hydrochloride), the hydrochloride salt of verubulin, is a quinazoline-based and BBB (blood brain barrier) permeable microtubule-disrupting agent with potential antitumor activity. It functions as a vascular disrupting agent (VDA) and is named as such because it destabilizes the polymerization of microtubules. It was undergoing clinical trials to treat glioblastoma (GBM).
| Targets |
microtubule
|
|---|---|
| ln Vitro |
Verubulin hydrochloride is the hydrochloride of compound Verubulin. With GI50 values of 3–6 nM in T47D, HCT116, and SNU-398 cells, verubulin (MPC-6827) is a strong inhibitor of cancer cell growth.[2]
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| ln Vivo |
Verubulin (MPC-6827) is effective in an MX-1 breast tumor model and has good blood-brain barrier penetration.[2]
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| References | |
| Additional Infomation |
Verubulin Hydrochloride is the hydrochloride salt form of verubulin, a quinazoline derivative with potential dual antineoplastic activities. Verubulin binds to and inhibits tubulin polymerization and interrupts microtubule formation, resulting in disruption of mitotic spindle assembly, cell cycle arrest in the G2/M phase, and cell death. This agent is not a substrate for several subtypes of multidrug resistance ABC transporters, such as P-glycoprotein, multidrug resistance-associated protein 1 (MRP1), and breast cancer resistance protein 1 (BCRP1); therefore, it may be useful for treating multidrug resistant (MDR) tumors that express these transporters. In addition, as a vascular disrupting agent (VDA), verubulin appears to disrupt tumor microvasculature specifically, which may result in acute ischemia and massive tumor cell death.
|
| Molecular Formula |
C₁₇H₁₈CLN₃O
|
|---|---|
| Molecular Weight |
315.80
|
| Exact Mass |
315.114
|
| Elemental Analysis |
C, 64.66; H, 5.75; Cl, 11.23; N, 13.31; O, 5.07
|
| CAS # |
917369-31-4
|
| Related CAS # |
Verubulin;827031-83-4
|
| PubChem CID |
11638255
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| Appearance |
White to light yellow solid powder
|
| LogP |
4.516
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
22
|
| Complexity |
330
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl.N1C2C(=CC=CC=2)C(N(C)C2C=CC(OC)=CC=2)=NC=1C
|
| InChi Key |
VYUWDIKZJLOZJL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H17N3O.ClH/c1-12-18-16-7-5-4-6-15(16)17(19-12)20(2)13-8-10-14(21-3)11-9-13;/h4-11H,1-3H3;1H
|
| Chemical Name |
N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine;hydrochloride
|
| Synonyms |
MPC-6827; MPC6827; MPC 6827; Verubulin HCl; Verubulin hydrochloride
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO 56~62.5 mg/mL (177.3~197.9 mM)
Ethanol: ~56 mg/mL (~177.3 mM) Water: ~56 mg/mL (~177.3 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.92 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 25.0 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: ≥ 2.5 mg/mL (7.92 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1666 mL | 15.8328 mL | 31.6656 mL | |
| 5 mM | 0.6333 mL | 3.1666 mL | 6.3331 mL | |
| 10 mM | 0.3167 mL | 1.5833 mL | 3.1666 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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