Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H30O4 |
Molecular Weight | 358.4712 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(C[C@H](C)[C@H](C)CC2=CC(OC)=C(OC)C=C2)C=C1OC
InChI
InChIKey=ORQFDHFZSMXRLM-IYBDPMFKSA-N
InChI=1S/C22H30O4/c1-15(11-17-7-9-19(23-3)21(13-17)25-5)16(2)12-18-8-10-20(24-4)22(14-18)26-6/h7-10,13-16H,11-12H2,1-6H3/t15-,16+
Temperocol is an investigative anti-cancer drug that inhibits the expression of survivin and CDK-1; discovered at Johns Hopkins University and under development by Erimos Pharmaceuticals. It has been tested in phase I/II clinical trials for Leukemia, and several forms of neoplasms including gliomas. Results of these clinical trials have shown promise, however treatment regimes produce several toxic side effects that need to be balanced against efficacy. Temperocol is a fully methylated derivative of the natural product Nordihydroguaiaretic acid.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: O15392|||Q75SP2 Gene ID: 332.0 Gene Symbol: BIRC5 Target Organism: Homo sapiens (Human) |
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Target ID: P06493 Gene ID: 983.0 Gene Symbol: CDK1 Target Organism: Homo sapiens (Human) |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
T1/2
Value | Dose | Co-administered | Analyte | Population |
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17.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18418294 |
750 mg 1 times / day multiple, intravenous dose: 750 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
TERAMEPROCOL serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Sample Use Guides
Terameprocol (EM-1421) was given as a single intravenous dose over 6 hours three times a week in a 3-week cycle of 2 weeks on, and one week off. Dosing began with 1000 mg and will be adjusted up or down to 500, 1500, and 2200 mg. Patients will continue in subsequent cycles until disease progression or until severe toxicities occur outweighing any benefits. Partial remission and transfusion independence were achieved in the 1500 mg cohort.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23299390
HCC2429 and H460 lung cancer cells were transfected with pLuc2931 luciferase reporter under the control of human survivin promoter fragment and pLuc control. Cells were cultured in RPMI1640 supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin and incubated in a 5% CO2 atmosphere at 37 deg-C. Cells were treated with 10 microM terameprocol and incubated for up to 48 hours. Downregulation of survivin transcription was noted at 24 hours and continued to increase to 48 hours.
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NCI_THESAURUS |
C1742
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NCI_THESAURUS |
C2161
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C61441
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C076852
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476861
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53YET703F2
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DB12226
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300000034412
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CHEMBL90983
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8860
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SS-63
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24150-24-1
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ACTIVE MOIETY