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MedKoo Cat#: 533447 | Name: DCZ0415
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

DCZ0415 is a novel inhibitor of TRIP13, suppressing multiple myeloma progression.

Chemical Structure

DCZ0415
DCZ0415
CAS#2242470-43-3

Theoretical Analysis

MedKoo Cat#: 533447

Name: DCZ0415

CAS#: 2242470-43-3

Chemical Formula: C23H20N2O2

Exact Mass: 356.1525

Molecular Weight: 356.43

Elemental Analysis: C, 77.51; H, 5.66; N, 7.86; O, 8.98

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to ship
10mg USD 250.00 Ready to ship
25mg USD 450.00 Ready to ship
50mg USD 750.00 Ready to ship
100mg USD 1,250.00 Ready to ship
200mg USD 1,950.00 Ready to ship
500mg USD 3,250.00 Ready to ship
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Related CAS #
No Data
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
More Info
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 mg/mL mM
Solubility
DMSO 62.5 175.35
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 356.43 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.

Recalculate based on batch purity %
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.
1: Agarwal S, Afaq F, Bajpai P, Kim HG, Elkholy A, Behring M, Chandrashekar DS, Diffalha SA, Khushman M, Sugandha SP, Varambally S, Manne U. DCZ0415, a small- molecule inhibitor targeting TRIP13, inhibits EMT and metastasis via inactivation of the FGFR4/STAT3 axis and the Wnt/β-catenin pathway in colorectal cancer. Mol Oncol. 2022 Apr;16(8):1728-1745. doi: 10.1002/1878-0261.13201. Epub 2022 Mar 7. PMID: 35194944; PMCID: PMC9019876. 2: Afaq F, Agarwal S, Bajpai P, Diffalha SA, Kim HG, Peter S, Khushman M, Chauhan SC, Mukherjee P, Varambally S, Manne U. Targeting of oncogenic AAA- ATPase TRIP13 reduces progression of pancreatic ductal adenocarcinoma. Neoplasia. 2024 Jan;47:100951. doi: 10.1016/j.neo.2023.100951. Epub 2023 Nov 30. PMID: 38039923; PMCID: PMC10716004. 3: 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. 4: Jacob Bunu S, Cai H, Wu L, Zhang H, Zhou Z, Xu Z, Shi J, Zhu W. TRIP13 - a potential drug target in cancer pharmacotherapy. Bioorg Chem. 2024 Oct;151:107650. doi: 10.1016/j.bioorg.2024.107650. Epub 2024 Jul 18. PMID: 39042962. 5: Hagihara Y, Tomioka Y, Suetsugu T, Shinmura M, Misono S, Goto Y, Kikkawa N, Kato M, Inoue H, Mizuno K, Seki N. Identification of Tumor-Suppressive miR-139-3p-Regulated Genes: TRIP13 as a Therapeutic Target in Lung Adenocarcinoma. Cancers (Basel). 2023 Nov 24;15(23):5571. doi: 10.3390/cancers15235571. PMID: 38067275; PMCID: PMC10705761. 6: Chen G, Gao X, Jia X, Wang Y, Xu L, Yu D, Chang S, Deng H, Hu K, Wang G, Li B, Xu Z, Lu Y, Wang H, Zhang T, Song D, Yang G, Wu X, Zhu H, Zhu W, Shi J. Ribosomal protein S3 mediates drug resistance of proteasome inhibitor: potential therapeutic application in multiple myeloma. Haematologica. 2024 Apr 1;109(4):1206-1219. doi: 10.3324/haematol.2023.282789. PMID: 37767568; PMCID: PMC10985453. 7: Xu H, Ma Z, Mo X, Chen X, Xu F, Wu F, Chen H, Zhou G, Xia H, Zhang C. Inducing Synergistic DNA Damage by TRIP13 and PARP1 Inhibitors Provides a Potential Treatment for Hepatocellular Carcinoma. J Cancer. 2022 Apr 11;13(7):2226-2237. doi: 10.7150/jca.66020. PMID: 35517402; PMCID: PMC9066198. 8: Dong S, Hu K, Shi Y, Wang G, Yu D, Zhao Y, Zhang H, Wang Y, Sun H, Xu Z, Jia Q, Li Y, Li Y, Li B, Shi J, Zhu W. Design and synthesis of cantharidin derivative DCZ5418 as a TRIP13 inhibitor with anti-multiple myeloma activity in vitro and in vivo. Bioorg Med Chem Lett. 2024 Jan 15;98:129590. doi: 10.1016/j.bmcl.2023.129590. Epub 2023 Dec 12. PMID: 38092072. 9: Li X, Zhang H, Dong S, Gao X, Sun H, Zhou Z, Hu K, Guo S, Zhang Q, Guo Z, Jacob Bunu S, Zhu J, Li B, Zhang Y, Shen J, Akber Aisa H, Xu Z, Cai H, Shi J, Zhu W. Design, synthesis, and biological evaluation of novel 1-amido-2-one-4-thio-deoxypyranose as potential antitumor agents for multiple myeloma. Bioorg Med Chem. 2024 Sep 1;111:117843. doi: 10.1016/j.bmc.2024.117843. Epub 2024 Jul 22. PMID: 39083980. 10: Chen Y, Chen D, Qin Y, Qiu C, Zhou Y, Dai M, Li L, Sun Q, Jiang Y. TRIP13, identified as a hub gene of tumor progression, is the target of microRNA-4693-5p and a potential therapeutic target for colorectal cancer. Cell Death Discov. 2022 Jan 24;8(1):35. doi: 10.1038/s41420-022-00824-w. PMID: 35075117; PMCID: PMC8786872.