Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H25ClFN5O3.2C4H4O4 |
| Molecular Weight | 706.072 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 2 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)\C=C\C(O)=O.OC(=O)\C=C\C(O)=O.CNC(=O)CN1CCC(CC1)OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC
InChI
InChIKey=LSXKPHWAKWZIKV-LVEZLNDCSA-N
InChI=1S/C23H25ClFN5O3.2C4H4O4/c1-26-21(31)12-30-8-6-14(7-9-30)33-20-10-15-18(11-19(20)32-2)27-13-28-23(15)29-17-5-3-4-16(24)22(17)25;2*5-3(6)1-2-4(7)8/h3-5,10-11,13-14H,6-9,12H2,1-2H3,(H,26,31)(H,27,28,29);2*1-2H,(H,5,6)(H,7,8)/b;2*2-1+
Sapitinib is an oral, reversible and equipotent inhibitor of EGFR, HER2 and HER3 signalling. The drug was tested in phase II of clinical trials in patients with breast cancer, colorectal cancer, gastric cancer and NSCL carcinoma, however its development for breast cancer therapy seems to be terminated. Sapitinib absorption is rapid and the drug is totally cleared by metabolism with the major routes being oxidation and amine or ether cleavage around the piperidine ring with subsequent glucuronide or sulphate conjugation.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL203 |
4.0 nM [IC50] | ||
Target ID: CHEMBL1824 |
3.0 nM [IC50] | ||
Target ID: CHEMBL5838 |
4.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| 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 |
Sample Use Guides
Colorectal cancer: Patients were receiving 160 mg sapitinib tablets, twice daily on days 1-4 of each 2-weekly cycle + FOLFIRI. Breast cancer: Patients were receiving daily anastrozole (1 mg) in combination with sapitinib 20 mg twice daily (bid) or sapitinib 40 mg bid.
Route of Administration:
Oral
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1196531-39-1
Created by
admin on Sat Dec 16 14:13:19 GMT 2023 , Edited by admin on Sat Dec 16 14:13:19 GMT 2023
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RD1QAE9R4N
Created by
admin on Sat Dec 16 14:13:19 GMT 2023 , Edited by admin on Sat Dec 16 14:13:19 GMT 2023
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44470103
Created by
admin on Sat Dec 16 14:13:19 GMT 2023 , Edited by admin on Sat Dec 16 14:13:19 GMT 2023
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PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD
