Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H18F2N4O3.ClH |
| Molecular Weight | 424.829 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN1C(=O)C(OC2=CC=C(F)C=C2F)=CC3=C1N=C(NC4CCOCC4)N=C3
InChI
InChIKey=RQHSAIGGUWVOBG-UHFFFAOYSA-N
InChI=1S/C19H18F2N4O3.ClH/c1-25-17-11(10-22-19(24-17)23-13-4-6-27-7-5-13)8-16(18(25)26)28-15-3-2-12(20)9-14(15)21;/h2-3,8-10,13H,4-7H2,1H3,(H,22,23,24);1H
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Q16539|||Q8TDX0 Gene ID: 1432.0 Gene Symbol: MAPK14 Target Organism: Homo sapiens (Human) |
0.2 nM [Kd] | ||
Target ID: P45984|||Q15711 Gene ID: 5601.0 Gene Symbol: MAPK9 Target Organism: Homo sapiens (Human) |
9.0 nM [Kd] | ||
Target ID: P53779 Gene ID: 5602.0 Gene Symbol: MAPK10 Target Organism: Homo sapiens (Human) |
3.0 nM [Kd] | ||
Target ID: Q9UBE8 Gene ID: 51701.0 Gene Symbol: NLK Target Organism: Homo sapiens (Human) |
6.0 nM [Kd] |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.65 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
1.56 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Macaca fascicularis population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.11 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Canis lupus population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.35 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
29.4 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Macaca fascicularis population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.31 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Canis lupus population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
22.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Macaca fascicularis population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.23 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Canis lupus population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
4.4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
4.6% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Macaca fascicularis population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
9.6% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21375264/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
R-1487 plasma | Canis lupus population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
| Name | Type | Language | ||
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Preferred Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Systematic Name | English | ||
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Systematic Name | English |
| Classification Tree | Code System | Code | ||
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MANUFACTURER PRODUCT INFORMATION |
6-(2,4-DIFLUOROPHENOXY)-8-METHYL-2-(TETRAHYDROPYRAN-4-YLAMINO)PYRIDO(2,3-D)PYRIMIDIN-7-ONE HYDROCHLORIDE
Created by
admin on Mon Mar 31 23:36:39 GMT 2025 , Edited by admin on Mon Mar 31 23:36:39 GMT 2025
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DTXSID60712354
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E89N7YW9YQ
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54580957
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449808-64-4
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admin on Mon Mar 31 23:36:39 GMT 2025 , Edited by admin on Mon Mar 31 23:36:39 GMT 2025
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ACTIVE MOIETY
SUBSTANCE RECORD
