WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 533447
CAS#: 2242470-43-3
Description: DCZ0415 is a novel inhibitor of TRIP13, suppressing multiple myeloma progression.
MedKoo Cat#: 533447
Name: DCZ0415
CAS#: 2242470-43-3
Chemical Formula: C23H20N2O2
Exact Mass: 356.1525
Molecular Weight: 356.425
Elemental Analysis: C, 77.51; H, 5.66; N, 7.86; O, 8.98
Synonym: DCZ0415; DCZ-0415; DCZ 0415;
IUPAC/Chemical Name: 2-(4-(Pyridin-4-ylmethyl)phenyl)-4,4a,5,5a,6,6a-hexahydro-4,6-ethenocyclopropa[f]isoindole-1,3(2H,3aH)-dione
InChi Key: LOXMLWHUIONWMI-UHFFFAOYSA-N
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
SMILES Code: O=C1N(C2=CC=C(CC3=CC=NC=C3)C=C2)C(C4C5C(C6)C6C(C=C5)C14)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. |
| In vitro activity: | To evaluate the inhibitory effect of DCZ0415, multiple myeloma cells were treated with DCZ0415 for 72 hours and cell viability was assessed. Data showed that DCZ0415 induced a significant dose-dependent decrease in viability (Fig. 3A). Reference: Cancer Res. 2020 Feb 1;80(3):536-548. https://cancerres.aacrjournals.org/content/80/3/536.long |
| In vivo activity: | To investigate the therapeutic potential of DCZ0415 in vivo, an multiple myeloma mouse xenograft model was employed. The administration of DCZ0415 significantly reduced the growth of multiple myeloma cells-induced tumors in immunodeficient mice compared with control mice (Fig. 7A). Reference: Cancer Res. 2020 Feb 1;80(3):536-548. https://cancerres.aacrjournals.org/content/80/3/536.long |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 62.5 | 175.35 |
The following data is based on the product molecular weight 356.425 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Wang Y, Huang J, Li B, Xue H, Tricot G, Hu L, Xu Z, Sun X, Chang S, Gao L, Tao Y, Xu H, Xie Y, Xiao W, Yu D, Kong Y, Chen G, Sun X, Lian F, Zhang N, Wu X, Mao Z, Zhan F, Zhu W, Shi J. A Small-Molecule Inhibitor Targeting TRIP13 Suppresses Multiple Myeloma Progression. Cancer Res. 2020 Feb 1;80(3):536-548. doi: 10.1158/0008-5472.CAN-18-3987. Epub 2019 Nov 15. PMID: 31732653. |
| In vitro protocol: | 1. Wang Y, Huang J, Li B, Xue H, Tricot G, Hu L, Xu Z, Sun X, Chang S, Gao L, Tao Y, Xu H, Xie Y, Xiao W, Yu D, Kong Y, Chen G, Sun X, Lian F, Zhang N, Wu X, Mao Z, Zhan F, Zhu W, Shi J. A Small-Molecule Inhibitor Targeting TRIP13 Suppresses Multiple Myeloma Progression. Cancer Res. 2020 Feb 1;80(3):536-548. doi: 10.1158/0008-5472.CAN-18-3987. Epub 2019 Nov 15. PMID: 31732653. |
| In vivo protocol: | 1. Wang Y, Huang J, Li B, Xue H, Tricot G, Hu L, Xu Z, Sun X, Chang S, Gao L, Tao Y, Xu H, Xie Y, Xiao W, Yu D, Kong Y, Chen G, Sun X, Lian F, Zhang N, Wu X, Mao Z, Zhan F, Zhu W, Shi J. A Small-Molecule Inhibitor Targeting TRIP13 Suppresses Multiple Myeloma Progression. Cancer Res. 2020 Feb 1;80(3):536-548. doi: 10.1158/0008-5472.CAN-18-3987. Epub 2019 Nov 15. PMID: 31732653. |
