Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C34H41FN4O4S2 |
| Molecular Weight | 652.842 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CSCC[C@H](NC(=O)C1=C(CCC2=CC=C(F)C=C2)C=CC(NC[C@@H]3C[C@@H](CN3)SC(=O)C4=CN=CC=C4)=C1)C(=O)OC(C)C
InChI
InChIKey=HKGUHEGKBLYKHY-QMOZSOIISA-N
InChI=1S/C34H41FN4O4S2/c1-22(2)43-33(41)31(14-16-44-3)39-32(40)30-18-27(13-10-24(30)9-6-23-7-11-26(35)12-8-23)37-20-28-17-29(21-38-28)45-34(42)25-5-4-15-36-19-25/h4-5,7-8,10-13,15,18-19,22,28-29,31,37-38H,6,9,14,16-17,20-21H2,1-3H3,(H,39,40)/t28-,29-,31-/m0/s1
Approval Year
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F99W9H5WUE
Created by
admin on Sat Dec 16 18:33:19 GMT 2023 , Edited by admin on Sat Dec 16 18:33:19 GMT 2023
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AZD-3409
Created by
admin on Sat Dec 16 18:33:19 GMT 2023 , Edited by admin on Sat Dec 16 18:33:19 GMT 2023
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PRIMARY | AZD3409 is a farnesyl-transferase inhibitor (FAR) indicated for the treatment of solid tumors. Phase I trials were initiated January 2003, and were ongoing as of February 2004. As of February 2007 the development of AZD3409 had been discontinued.AZD3409 is a novel, oral, antitumor agent that acts as a prenyl transferase inhibitor. It has potentially broad antitumor activity both as monotherapy and in combination with other anticancer treatments. AZD3409 is a double pro-drugits metabolism involves conversion to a thiol-ester intermediate, then, intracellularly, to a thiol-acid active species. Phase I trials were initiated January 2003, and were ongoing as of February 2004. Recent studies have shown that AZD3409 is a potent inhibitor of both prostate epithelial cell proliferation and cellular invasion, without an associated bone marrow cellular toxicity.In preclinical studies, AZD3409 achieves up to 90% inhibition of FTase in tumors at well tolerated doses. In enzyme studies AZD3409 is also known to inhibit GGTase-1. | ||
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11377266
Created by
admin on Sat Dec 16 18:33:19 GMT 2023 , Edited by admin on Sat Dec 16 18:33:19 GMT 2023
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345915-10-8
Created by
admin on Sat Dec 16 18:33:19 GMT 2023 , Edited by admin on Sat Dec 16 18:33:19 GMT 2023
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PRIMARY | |||
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AZD-3409
Created by
admin on Sat Dec 16 18:33:19 GMT 2023 , Edited by admin on Sat Dec 16 18:33:19 GMT 2023
|
PRIMARY | Description: AZD-3409 is a potent prenyl transferase inhibitor. AZD-3409 showed higher potency than lonafarnib. The mean IC(50) for cytotoxicity of AZD3409 was 510 in MEF cells, 10,600 in A549 cells and 6,170 in MCF7 cells, respectively. In these cells, the IC(50) for FTase activity of AZD3409 ranged from 3.0 to 14.2 nM and of lonafarnib from 0.26 to 31.3 nM. AZD3409 inhibits farnesylation to a higher extent than geranylgeranylation. Both inhibition of farnesylation and geranylgeranylation could not be correlated to the antiproliferative activity of the drug. AZD3409 might be active in gefitinib-resistant breast carcinoma. (Last update: 7/9/2015). |
ACTIVE MOIETY
METABOLITE (PARENT)
SALT/SOLVATE (PARENT)
SUBSTANCE RECORD
