Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H27F3N4O3 |
| Molecular Weight | 464.4807 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1(C)CC2=C(C(=NN2C3=CC=C(C(N)=O)C(N[C@H]4CC[C@H](O)CC4)=C3)C(F)(F)F)C(=O)C1
InChI
InChIKey=ZFVRYNYOPQZKDG-MQMHXKEQSA-N
InChI=1S/C23H27F3N4O3/c1-22(2)10-17-19(18(32)11-22)20(23(24,25)26)29-30(17)13-5-8-15(21(27)33)16(9-13)28-12-3-6-14(31)7-4-12/h5,8-9,12,14,28,31H,3-4,6-7,10-11H2,1-2H3,(H2,27,33)/t12-,14-
| Molecular Formula | C23H27F3N4O3 |
| Molecular Weight | 464.4807 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
SNX-2112, a novel 2-aminobenzamide inhibitor of heat shock protein 90 (Hsp90) was discovered by Serenex. This drug was investigated for treatment of different cancer cell lines, including hepatocellular carcinoma cells, breast cancer cells and in combination with 5-fluorouracil in esophageal cancer. However, subsequent development has been discontinued due to ocular toxicity as identified in a phase I study.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. | 2008 Jan 1 |
|
| Targeting of multiple signaling pathways by the Hsp90 inhibitor SNX-2112 in EGFR resistance models as a single agent or in combination with erlotinib. | 2009 |
|
| Antitumor activity of SNX-2112, a synthetic heat shock protein-90 inhibitor, in MET-amplified tumor cells with or without resistance to selective MET Inhibition. | 2011 Jan 1 |
Sample Use Guides
Treatment of BT-474 cells with 1 μM SNX-2112 results in down-regulation of HER2 expression. Treatment with SNX-2112 also results in a decline in total Akt expression. SNX-2112 inhibits cell proliferation with IC50 values ranging from 10 to 50 nM, in BT474, SKBR-3, SKOV-3, MDA-468, MCF-7 and H1650 cancer cells. And these antiproliferative effects are associated with hypophosphorylation of Rb, arrest of G1 and modest levels of apotosis.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 02:44:31 UTC 2023
by
admin
on
Sat Dec 16 02:44:31 UTC 2023
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| Record UNII |
10C9P3FFOW
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| Record Status |
Validated (UNII)
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| Record Version |
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24772860
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10C9P3FFOW
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DTXSID601025695
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