U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C22H24FN5O4
Molecular Weight 441.4555
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SUPINOXIN

SMILES

COC1=CC(OC)=CC(=C1)N2CCN(CC2)C(=O)NC3=C(OC)N=C4C=CC(F)=CC4=N3

InChI

InChIKey=KAKPGJJRYRYSTP-UHFFFAOYSA-N
InChI=1S/C22H24FN5O4/c1-30-16-11-15(12-17(13-16)31-2)27-6-8-28(9-7-27)22(29)26-20-21(32-3)25-18-5-4-14(23)10-19(18)24-20/h4-5,10-13H,6-9H2,1-3H3,(H,24,26,29)

HIDE SMILES / InChI

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Probable ATP-dependent RNA helicase DDX5
1
Target ID: P17844
Gene ID: 1655.0
Gene Symbol: DDX5
Target Organism: Homo sapiens (Human)
Inhibitor
8504
 61.0 nM [IC50]
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
252 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
226 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
364 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
225 mg single, oral
dose: 225 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
385 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
660 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
425 mg single, oral
dose: 425 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
707 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
575 mg single, oral
dose: 575 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
571 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
775 mg single, oral
dose: 775 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
394 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
403 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
250 mg 3 times / week multiple, oral
dose: 250 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
288 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
301 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
300 mg 3 times / week multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
347 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
150 mg 5 times / week multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
337 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
440 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
200 mg 5 times / week multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
498 μg/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
300.02 mg 5 times / week multiple, oral
dose: 300.02 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
2341 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3280 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
4312 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
225 mg single, oral
dose: 225 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
5847 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
14673 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
425 mg single, oral
dose: 425 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
10098 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
575 mg single, oral
dose: 575 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
6570 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
775 mg single, oral
dose: 775 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5211 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
7774 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
250 mg 3 times / week multiple, oral
dose: 250 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
4555 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
4143 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
300 mg 3 times / week multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3721 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
150 mg 5 times / week multiple, oral
dose: 150 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2752 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
4034 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
200 mg 5 times / week multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
4359 μg × h/L
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
300.02 mg 5 times / week multiple, oral
dose: 300.02 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
11.4 h
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
12 h
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
225 mg single, oral
dose: 225 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
16 h
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
14 h
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
10.3 h
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
8.5 h
OTHER
https://d1io3yog0oux5.cloudfront.net/_8292ed9746f28d0168daa291af3fad3d/rexahn/db/432/3239/pdf/2016_June_ASCO+RX-5902+FINAL+poster.pdf
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SUPINOXIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Name Type Language
SUPINOXIN
Common Name English
RX-5902
Preferred Name English
1-(3,5-DIMETHOXYPHENYL)-4-((6-FLUORO-2-METHOXYQUINOXALIN-3-YL)AMINOCARBONYL) PIPERAZINE
Systematic Name English
P-P68 INHIBITOR RX-5902
Common Name English
4-(3,5-DIMETHOXYPHENYL)-N-(7-FLUORO-3-METHOXY-QUINOXALIN-2-YL)PIPERAZINE-1-CARBOXAMIDE
Systematic Name English
1-PIPERAZINECARBOXAMIDE, 4-(3,5-DIMETHOXYPHENYL)-N-(7-FLUORO-3-METHOXY-2-QUINOXALINYL)-
Systematic Name English
Code System Code Type Description
NCI_THESAURUS
C113293
Created by admin on Tue Apr 01 16:39:11 GMT 2025 , Edited by admin on Tue Apr 01 16:39:11 GMT 2025
PRIMARY NCIT
CAS
888478-45-3
Created by admin on Tue Apr 01 16:39:11 GMT 2025 , Edited by admin on Tue Apr 01 16:39:11 GMT 2025
PRIMARY
PUBCHEM
11619093
Created by admin on Tue Apr 01 16:39:11 GMT 2025 , Edited by admin on Tue Apr 01 16:39:11 GMT 2025
PRIMARY
FDA UNII
ZU8OM8V5WF
Created by admin on Tue Apr 01 16:39:11 GMT 2025 , Edited by admin on Tue Apr 01 16:39:11 GMT 2025
PRIMARY
MANUFACTURER PRODUCT INFORMATION
SUPINOXIN
Created by admin on Tue Apr 01 16:39:11 GMT 2025 , Edited by admin on Tue Apr 01 16:39:11 GMT 2025
PRIMARY Description: Supinoxin, also known as RX-5902, is orally bioavailable small molecule inhibitor of phosphorylated-p68 RNA helicase (P-p68), with potential anti-proliferative and antineoplastic activity. Upon oral administration, P-p68 inhibitor RX-5902 may both inhibit the activity of the anti-apoptotic B-cell lymphoma 2 (Bcl-2) protein and facilitate the induction of cyclin-dependent kinase inhibitor 1 (p21). This may prevent G2/M cell cycle progression and lead to growth inhibition in tumor cells. P-p68 is overexpressed in various types of solid tumors but absent in normal tissues, and plays a role in tumor progression and metastasis. (last updated: 5/1/2016)
ACTIVE MOIETY
Structure of SUPINOXIN
NIH
NCATS
PRIVACY NOTICE
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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