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DCZ0415 (DCZ-0415; DCZ 0415) is a novel and highly potent TRIP13 inhibitor that is able to impair nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.
Targets |
NF-κB
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ln Vitro |
Colony formation is significantly reduced in response to DCZ0415 (10, 20 μM; 72 hours), which suggests that it inhibits cell proliferation[1].
In MM cells, DCZ0415 (1.25–40 μM; 72 hours) causes a significant dose-dependent reduction in viability[1]. Treatment with DCZ0415 (10, 20 μM; 24-72 hours) elicits apoptotic cell death in a dose-dependent manner[1]. In G0/G1 MM cells, DCZ0415 (10, 20 μM; 24 hours) induces a sizable accumulation[1]. In MM cells, DCZ0415 (10 μM; 48 hours) reduces the levels of phosphorylated (p)-iB and phosphorylated (p)-NF-B proteins[1]. In CalcuSyn in MM cell lines, DCZ0415 has IC50 values of 1.0–10 μM[1]. In MM cells, DCZ0415 inhibits the synthesis of DNA 288 to cause cytotoxic effects[1]. |
ln Vivo |
In immune-deficient mice, DCZ0415 (ip; 50 mg/kg/day for 14 days) significantly slows the growth of tumors brought on by MM cells[1].
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Animal Protocol |
Nude mice (6-weeks-old) with H929 775 cells[1]
50 mg/kg Intraperitoneal injection; every day for 14 days |
References |
Molecular Formula |
C23H20N2O2
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Molecular Weight |
356.4171
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Exact Mass |
356.15
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Elemental Analysis |
C, 77.51; H, 5.66; N, 7.86; O, 8.98
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CAS # |
2242470-43-3
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Related CAS # |
2242470-43-3
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Appearance |
Solid powder
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SMILES |
C1C2C1C3C=CC2C4C3C(=O)N(C4=O)C5=CC=C(C=C5)CC6=CC=NC=C6
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InChi Key |
LOXMLWHUIONWMI-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C23H20N2O2/c26-22-20-16-5-6-17(19-12-18(16)19)21(20)23(27)25(22)15-3-1-13(2-4-15)11-14-7-9-24-10-8-14/h1-10,16-21H,11-12H2
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Chemical Name |
4-[4-(pyridin-4-ylmethyl)phenyl]-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-ene-3,5-dione
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Synonyms |
DCZ 0415; DCZ0415; DCZ-0415
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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: ~62.5 mg/mL (~175.4 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.84 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 20.8 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: ≥ 2.08 mg/mL (5.84 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8057 mL | 14.0284 mL | 28.0568 mL | |
5 mM | 0.5611 mL | 2.8057 mL | 5.6114 mL | |
10 mM | 0.2806 mL | 1.4028 mL | 2.8057 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.
Binding of DCZ0415 to TRIP13. Cancer Res . 2020 Feb 1;80(3):536-548. td> |
DCZ0415 inhibits the proliferation of multiple myeloma cell lines and induces apoptosis. Cancer Res . 2020 Feb 1;80(3):536-548. td> |
The anti-MM activity of DCZ0415 depends on TRIP13. Cancer Res . 2020 Feb 1;80(3):536-548. td> |
DCZ0415 impaired DNA repair and inhibited NF-κB activity in multiple myeloma cells. Cancer Res . 2020 Feb 1;80(3):536-548. td> |