Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C24H33N3O4 |
| Molecular Weight | 427.5365 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)CCCNC(=O)C(\COC1=C2C=CC=CC2=CC=C1)=C\CCCCC(=O)NO
InChI
InChIKey=AUGCSOFQTDKPSO-RGVLZGJSSA-N
InChI=1S/C24H33N3O4/c1-27(2)17-9-16-25-24(29)20(11-4-3-5-15-23(28)26-30)18-31-22-14-8-12-19-10-6-7-13-21(19)22/h6-8,10-14,30H,3-5,9,15-18H2,1-2H3,(H,25,29)(H,26,28)/b20-11+
CG-200745 is a novel inhibitor of histone deacetylases (HDACs), initially developed by CrystalGenomics, Inc for treatment of various hematological and solid cancers. Combinations of CG-200745 with SN38 (the active form of irinotecan), or oxaliplatin were more effective than the agents alone when used to inhibit the growth of HCT116 cells. The protein expressions of acetyl-H3, p21, caspase-3, -8, and -9, PARP, and XIAP were affected in a time- and dose-dependent manner in HCT116 cells treated with the CG-200745 alone or combined CG-200745 and SN-38. In HCT116 xenografts, the HDACI CG-200745 in combination with irinotecan dramatically inhibited tumor growth without showing additive toxicity.
Approval Year
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| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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FDA ORPHAN DRUG |
919022
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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FDA ORPHAN DRUG |
760420
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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FDA ORPHAN DRUG |
846121
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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FDA ORPHAN DRUG |
793520
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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DTXSID801028069
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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300000010881
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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16117309
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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936221-33-9
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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CG-200745
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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PRIMARY | Description: CG200745 is a novel hydroxamate-based pan-histone deacetylase inhibitor (HDACI). Like other inhibitors, CG200745 has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. CG200745 inhibited deacetylation of histone H3 and tubulin as much as vorinostat and belinostat did. CG200745 also inhibited growth of prostate cancer cells, increased sub-G1 population, and activated caspase-9, -3 and -8 in LNCaP, DU145 and PC3 cells. These results indicate that CG200745 induces apoptosis. The preclinical results show that combination treatment with docetaxel and new HDACI, CG200745, potentiated anti-tumor effect in hormone-refractory prostate cancer (HRPC) cells via activation of apoptosis. (Last update: 5/30/2016). | ||
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HDCG-0745
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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PRIMARY | Official Title: A Phase I/II Study of Combination Therapy of CG200745 PPA With Gemcitabine and Erlotinib to Determine the Maximum Tolerated Dose (MTD) and Evaluate the Safety and Efficacy for Locally Advanced Unresectable, or Metastatic Pancreatic Cancer.The phase I clinical trial is to identify the MTD (Maximum Tolerated Dose) and DLT (Dose Limiting Toxicity) of CG200745 PPA in combination use of Gemcitabine and Erlotinib. Initial dose of CG200745 PPA is 187.5 mg/m^2, and it will be extended to 250 mg/m^2, 312.5 mg/m^2 or it will be reduced to 125 mg/m^2 based on the results of the cohort of 3 subjects per dose level.In the phase II clinical trial, the subjects will be administered with the dose which is to be identified as a recommended dose based on the results of Phase I study. The whole one cycle is consisted of 28 days, same as the phase I. The entire treatment period is 6 cycles and tumor assessment is evaluated every 2 cycles. | ||
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DB12259
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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11072
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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CG-200745
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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PRIMARY | Official Title: A Phase I/II Study of CG200745 PPA to Determine the Maximum Tolerated Dose and Evaluate the Safety and Efficacy in Patients With Myelodysplastic Syndrome (MDS) Who Failed to Respond to Prior Hypomethylating Therapy | ||
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C94225
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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4I8MLM7L2H
Created by
admin on Sat Dec 16 11:09:17 GMT 2023 , Edited by admin on Sat Dec 16 11:09:17 GMT 2023
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
