| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
|
| Targets |
IC50: 2.9 μM (VDR)[1].
|
|---|---|
| ln Vitro |
MeTC7 (compound 5) has an IC50 value of 2.9 μM, indicating strong VDR inhibitory activity[1]. The VDR-Ligand-binding domain in Silico is disrupted by MeTC7[1]. In the ovarian cancer cell-line, MeTC7 (250 nM; 18 h) decreases the expressions of Importin-4 and RXRα[1]. MeTC7 (250 nM; 18 h) causes PARP1 cleavage and reduces the viability of ovarian cancer cells[1].
|
| ln Vivo |
MeTC7 (compound 5) (meTC7; 10 mg/kg) inhibits the growth of xenografts and spontaneous transgenic TH-MYCN neuroblastoma in vivo[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: 2008 cells Tested Tested Concentrations: 250 nM Incubation Duration: 18, 12 h Experimental Results: diminished the expression of RXR-α, Importin-4 and increased cleaved PARP1 expression in 2008 cells. Cell Viability Assay[1] Cell Types: SKOV-3, IGROV-1, CAOV-3, OVCAR-3, OVCAR-8, and 2008 ovarian cancer cell-lines Tested Tested Concentrations: 0, 0.25, 0.5, 0.75, 1.0, 1.25 μM Incubation Duration: 24 h Experimental Results: diminished the viability of SKOV-3, IGROV-1, CAOV- 3, OVCAR-3, OVCAR-8, and 2008 ovarian cancer cell-lines. |
| Animal Protocol |
Animal/Disease Models: Mice[1]
Doses: 10 mg/kg Route of Administration: IP Experimental Results: decreased the growth of xenografts derived from ovarian cancer, medulloblastoma, and pancreatic cancer cells. Inhibited the growth of neuroblastoma cells and Xenografts. decreased MYCN expression and blocked the growth of TH-MYCN transgene-driven spontaneous neuroblastoma. |
| References |
| Molecular Formula |
C32H48BRN3O4
|
|---|---|
| Molecular Weight |
618.645228385925
|
| Exact Mass |
617.282
|
| CAS # |
1817841-22-7
|
| PubChem CID |
165437232
|
| Appearance |
White to off-white solid powder
|
| LogP |
8
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
40
|
| Complexity |
1130
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
BrCC(=O)O[C@H]1CC[C@@]2(C)C3(C1)C=CC1([C@@H]4CC[C@H]([C@H](C)CCCC(C)C)[C@@]4(C)CC[C@@H]12)N1C(N(C)C(N13)=O)=O
|
| InChi Key |
LBFDLJSQMPCWKK-YMNKQYQVSA-N
|
| InChi Code |
InChI=1S/C32H48BrN3O4/c1-20(2)8-7-9-21(3)23-10-11-24-29(23,4)14-13-25-30(5)15-12-22(40-26(37)19-33)18-31(30)16-17-32(24,25)36-28(39)34(6)27(38)35(31)36/h16-17,20-25H,7-15,18-19H2,1-6H3/t21-,22+,23-,24-,25-,29-,30-,31?,32?/m1/s1
|
| Chemical Name |
[(2R,5R,6R,9R,10R,13S)-6,10,18-trimethyl-5-[(2R)-6-methylheptan-2-yl]-17,19-dioxo-16,18,20-triazahexacyclo[13.5.2.01,9.02,6.010,15.016,20]docos-21-en-13-yl] 2-bromoacetate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 16.67 mg/mL (26.95 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (2.70 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 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6164 mL | 8.0821 mL | 16.1642 mL | |
| 5 mM | 0.3233 mL | 1.6164 mL | 3.2328 mL | |
| 10 mM | 0.1616 mL | 0.8082 mL | 1.6164 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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