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Details

Stereochemistry RACEMIC
Molecular Formula C17H12ClN2O4.Na
Molecular Weight 366.731
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of XK-469

SMILES

[Na+].CC(OC1=CC=C(OC2=NC3=CC(Cl)=CC=C3N=C2)C=C1)C([O-])=O

InChI

InChIKey=OJENKXNXJPNEPU-UHFFFAOYSA-M
InChI=1S/C17H13ClN2O4.Na/c1-10(17(21)22)23-12-3-5-13(6-4-12)24-16-9-19-14-7-2-11(18)8-15(14)20-16;/h2-10H,1H3,(H,21,22);/q;+1/p-1

HIDE SMILES / InChI

Molecular Formula Na
Molecular Weight 22.9898
Charge 1
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C17H12ClN2O4
Molecular Weight 343.741
Charge -1
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

XK-469 (NSC 697887) is a synthetic quinoxaline phenoxypropionic acid derivative that possesses unusual solid tumor selectivity and activity against multidrug-resistant cancer cells. XK469 acts as a selective topoisomerase IIβ inhibitor. Other proposed mechanisms include XK469-induced inhibition of cyclin B1 ubiquitination and apoptosis via binding of the peripheral benzodiazepine receptor. A phase I study was performed to determine the safety and pharmacokinetics of XK469R in patients with various neoplasms.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
160.0 µM [IC50]
Target ID: Cyclin B1 ubiquitination
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
152 μg/mL
260 mg/m² 1 times / day multiple, intravenous
dose: 260 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
84.6 μg/mL
260 mg single, intravenous
dose: 260 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
264 μg/mL
2750 mg 3 times / week multiple, intravenous
dose: 2750 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
211 μg/mL
1750 mg 3 times / week multiple, intravenous
dose: 1750 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
2312 μg × h/mL
260 mg/m² 1 times / day multiple, intravenous
dose: 260 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
955 μg × h/mL
260 mg single, intravenous
dose: 260 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
14863 μg × h/mL
2750 mg 3 times / week multiple, intravenous
dose: 2750 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
9150 μg × h/mL
1750 mg 3 times / week multiple, intravenous
dose: 1750 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
53.9 h
260 mg/m² 1 times / day multiple, intravenous
dose: 260 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
55 h
2750 mg 3 times / week multiple, intravenous
dose: 2750 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
45 h
1750 mg 3 times / week multiple, intravenous
dose: 1750 mg
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
XK-469 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.7%
unknown, unknown
XK-469 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
2750 mg 3 times / 3 weeks multiple, intravenous (unknown)
Highest studied dose
Dose: 2750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
DLT: Hyperbilirubinemia, Mucositis...
Other AEs: Vomiting, Diarrhea...
Dose limiting toxicities:
Hyperbilirubinemia (1 pt)
Mucositis (grade 3, 2 patients)
Other AEs:
Vomiting (grade 2, 1 pt)
Diarrhea (grade 3, 1 pt)
Alopecia (grade 1, 1 pt)
Rash (grade 3, 1 pt)
Anorexia (grade 3, 1 pt)
Nausea (grade 3, 1 pt)
Sources:
260 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 260 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 260 mg/m2, 1 times / day
Sources:
unhealthy
n = 6
Health Status: unhealthy
Condition: solid tumours
Sex: M+F
Food Status: UNKNOWN
Population Size: 6
Sources:
DLT: neutropenia...
Other AEs: Nausea and vomiting, Fatigue...
Dose limiting toxicities:
neutropenia (grade 4, 1 pt)
Other AEs:
Nausea and vomiting (grade 1, 4 patients)
Fatigue (grade 3, 1 pt)
anemia (grade 2, 1 pt)
Sources:
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Other AEs: Diarrhea, Aspartate aminotransferase increase...
Other AEs:
Diarrhea (grade 1, 3 patients)
Aspartate aminotransferase increase (grade 2, 1 pt)
Alanine aminotransferase increase (grade 2, 1 pt)
Anorexia (grade 1, 2 patients)
Mucositis (grade 1, 2 patients)
Rash (grade 1, 1 pt)
Alopecia (grade 2, 1 pt)
Vomiting (grade 1, 4 patients)
Indigestion (grade 1, 1 pt)
Nausea (grade 2, 1 pt)
Dysgeusia (grade 1, 1 pt)
Sources:
2200 mg 3 times / 3 weeks multiple, intravenous
Studied dose
Dose: 2200 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2200 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
DLT: mucositis...
Other AEs: Anorexia, Alopecia...
Dose limiting toxicities:
mucositis (1 pt)
Other AEs:
Anorexia (grade 2, 1 pt)
Alopecia (grade 2, 1 pt)
Nausea (grade 3, 1 pt)
Aspartate aminotransferase increase (grade 1, 1 pt)
Vomiting (grade 2, 2 patients)
Rash (grade 2, 1 pt)
Sources:
346 mg/m2 1 times / day multiple, intravenous (unknown)
Studied dose
Dose: 346 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 346 mg/m2, 1 times / day
Sources:
unhealthy
n = 2
Health Status: unhealthy
Condition: solid tumours
Sex: unknown
Food Status: UNKNOWN
Population Size: 2
Sources:
DLT: Febrile neutropenia, infection...
Other AEs: anemia...
Dose limiting toxicities:
Febrile neutropenia (1 pt)
infection (grade 3, 1 pt)
Other AEs:
anemia (grade 1, 1 pt)
Sources:
AEs

AEs

AESignificanceDosePopulation
Hyperbilirubinemia 1 pt
DLT
2750 mg 3 times / 3 weeks multiple, intravenous (unknown)
Highest studied dose
Dose: 2750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Alopecia grade 1, 1 pt
2750 mg 3 times / 3 weeks multiple, intravenous (unknown)
Highest studied dose
Dose: 2750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Vomiting grade 2, 1 pt
2750 mg 3 times / 3 weeks multiple, intravenous (unknown)
Highest studied dose
Dose: 2750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Anorexia grade 3, 1 pt
2750 mg 3 times / 3 weeks multiple, intravenous (unknown)
Highest studied dose
Dose: 2750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Diarrhea grade 3, 1 pt
2750 mg 3 times / 3 weeks multiple, intravenous (unknown)
Highest studied dose
Dose: 2750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Nausea grade 3, 1 pt
2750 mg 3 times / 3 weeks multiple, intravenous (unknown)
Highest studied dose
Dose: 2750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Rash grade 3, 1 pt
2750 mg 3 times / 3 weeks multiple, intravenous (unknown)
Highest studied dose
Dose: 2750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Mucositis grade 3, 2 patients
DLT
2750 mg 3 times / 3 weeks multiple, intravenous (unknown)
Highest studied dose
Dose: 2750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Nausea and vomiting grade 1, 4 patients
260 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 260 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 260 mg/m2, 1 times / day
Sources:
unhealthy
n = 6
Health Status: unhealthy
Condition: solid tumours
Sex: M+F
Food Status: UNKNOWN
Population Size: 6
Sources:
anemia grade 2, 1 pt
260 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 260 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 260 mg/m2, 1 times / day
Sources:
unhealthy
n = 6
Health Status: unhealthy
Condition: solid tumours
Sex: M+F
Food Status: UNKNOWN
Population Size: 6
Sources:
Fatigue grade 3, 1 pt
260 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 260 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 260 mg/m2, 1 times / day
Sources:
unhealthy
n = 6
Health Status: unhealthy
Condition: solid tumours
Sex: M+F
Food Status: UNKNOWN
Population Size: 6
Sources:
neutropenia grade 4, 1 pt
DLT
260 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 260 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 260 mg/m2, 1 times / day
Sources:
unhealthy
n = 6
Health Status: unhealthy
Condition: solid tumours
Sex: M+F
Food Status: UNKNOWN
Population Size: 6
Sources:
Dysgeusia grade 1, 1 pt
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Indigestion grade 1, 1 pt
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Rash grade 1, 1 pt
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Anorexia grade 1, 2 patients
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Mucositis grade 1, 2 patients
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Diarrhea grade 1, 3 patients
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Vomiting grade 1, 4 patients
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Alanine aminotransferase increase grade 2, 1 pt
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Alopecia grade 2, 1 pt
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Aspartate aminotransferase increase grade 2, 1 pt
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
Nausea grade 2, 1 pt
1750 mg 3 times / 3 weeks multiple, intravenous (total daily dose)
RP2D
Dose: 1750 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 1750 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 12
Sources:
mucositis 1 pt
DLT
2200 mg 3 times / 3 weeks multiple, intravenous
Studied dose
Dose: 2200 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2200 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Aspartate aminotransferase increase grade 1, 1 pt
2200 mg 3 times / 3 weeks multiple, intravenous
Studied dose
Dose: 2200 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2200 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Alopecia grade 2, 1 pt
2200 mg 3 times / 3 weeks multiple, intravenous
Studied dose
Dose: 2200 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2200 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Anorexia grade 2, 1 pt
2200 mg 3 times / 3 weeks multiple, intravenous
Studied dose
Dose: 2200 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2200 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Rash grade 2, 1 pt
2200 mg 3 times / 3 weeks multiple, intravenous
Studied dose
Dose: 2200 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2200 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Vomiting grade 2, 2 patients
2200 mg 3 times / 3 weeks multiple, intravenous
Studied dose
Dose: 2200 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2200 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Nausea grade 3, 1 pt
2200 mg 3 times / 3 weeks multiple, intravenous
Studied dose
Dose: 2200 mg, 3 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 2200 mg, 3 times / 3 weeks
Sources:
unhealthy
n = 14
Health Status: unhealthy
Condition: acute leukemia
Sex: M+F
Food Status: UNKNOWN
Population Size: 14
Sources:
Febrile neutropenia 1 pt
DLT
346 mg/m2 1 times / day multiple, intravenous (unknown)
Studied dose
Dose: 346 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 346 mg/m2, 1 times / day
Sources:
unhealthy
n = 2
Health Status: unhealthy
Condition: solid tumours
Sex: unknown
Food Status: UNKNOWN
Population Size: 2
Sources:
anemia grade 1, 1 pt
346 mg/m2 1 times / day multiple, intravenous (unknown)
Studied dose
Dose: 346 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 346 mg/m2, 1 times / day
Sources:
unhealthy
n = 2
Health Status: unhealthy
Condition: solid tumours
Sex: unknown
Food Status: UNKNOWN
Population Size: 2
Sources:
infection grade 3, 1 pt
DLT
346 mg/m2 1 times / day multiple, intravenous (unknown)
Studied dose
Dose: 346 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 346 mg/m2, 1 times / day
Sources:
unhealthy
n = 2
Health Status: unhealthy
Condition: solid tumours
Sex: unknown
Food Status: UNKNOWN
Population Size: 2
Sources:
PubMed

PubMed

TitleDatePubMed
The investigational new drug XK469 induces G(2)-M cell cycle arrest by p53-dependent and -independent pathways.
2001 Nov
II. Synthesis and biological evaluation of some bioisosteres and congeners of the antitumor agent, 2-(4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy)propionic acid (XK469).
2002 Jul 4
Synthesis and biological evaluation of conformationally constrained analogs of the antitumor agents XK469 and SH80. Part 5.
2006 Apr 1
The role of autophagy in the death of L1210 leukemia cells initiated by the new antitumor agents, XK469 and SH80.
2007 Jan
Patents

Patents

Sample Use Guides

XK469 was administered on days 1–5 of a 21 day cycle. Dose 260 mg/m2/day was defined as the maximum tolerated dose.
Route of Administration: Intravenous
Induction of the Bax protein was insignificant when cells were exposed to 2 uM XK469, and there was no down-regulation of the Bcl-2 protein at 48 or 72 h. However, 5 uM XK469 induced Bax protein expression by 48 and 72 h and caused a decrease in constitutive levels of Bcl-2 by 72 h compared with control untreated cells. The Bax:Bcl-2 ratio was 11-fold in favor of Bax with 5 uM XK469.
Substance Class Chemical
Created
by admin
on Sat Dec 16 08:25:49 UTC 2023
Edited
by admin
on Sat Dec 16 08:25:49 UTC 2023
Record UNII
G6S5600O0D
Record Status Validated (UNII)
Record Version
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Name Type Language
XK-469
Common Name English
PROPANOIC ACID, 2-(4-((7-CHLORO-2-QUINOXALINYL)OXY)PHENOXY)-, SODIUM SALT
Systematic Name English
XK 469 [WHO-DD]
Common Name English
NSC-656889
Code English
XB-469
Common Name English
PROPANOIC ACID, 2-(4-((7-CHLORO-2-QUINOXALINYL)OXY)PHENOXY)-, SODIUM SALT, (±)-
Common Name English
Code System Code Type Description
EPA CompTox
DTXSID70935673
Created by admin on Sat Dec 16 08:25:49 UTC 2023 , Edited by admin on Sat Dec 16 08:25:49 UTC 2023
PRIMARY
CAS
157434-99-6
Created by admin on Sat Dec 16 08:25:49 UTC 2023 , Edited by admin on Sat Dec 16 08:25:49 UTC 2023
PRIMARY
FDA UNII
G6S5600O0D
Created by admin on Sat Dec 16 08:25:49 UTC 2023 , Edited by admin on Sat Dec 16 08:25:49 UTC 2023
PRIMARY
PUBCHEM
23675947
Created by admin on Sat Dec 16 08:25:49 UTC 2023 , Edited by admin on Sat Dec 16 08:25:49 UTC 2023
PRIMARY
NSC
656889
Created by admin on Sat Dec 16 08:25:49 UTC 2023 , Edited by admin on Sat Dec 16 08:25:49 UTC 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY