Drug Information

Drug (ID: DG01516) and It's Reported Resistant Information
Name
Sapitinib
Synonyms
Sapitinib; 848942-61-0; AZD8931; AZD-8931; AZD8931 (Sapitinib); 2-(4-((4-((3-Chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)-n-methylacetamide; Sapitinib(AZD8931); Sapitinib (AZD-8931); UNII-3499328002; CHEMBL2408045; 2-[4-({4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}oxy)piperidin-1-yl]-N-methylacetamide; 2-[4-[4-(3-chloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]-N-methylacetamide; Sapitinib [INN]; 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-((1-(n-methylcarbamoylmethyl)piperidin-4-yl)oxy)quinazoline; 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-[[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy]quinazoline; Sapitinib [WHO-DD]; sapitinibum; AZD 8931; AZD-8931(Sapitinib); Sapitinib (AZD8931); MLS006011283; SCHEMBL202358; GTPL7717; DTXSID50233942; EX-A036; CHEBI:132986; BCPP000365; HMS3655J08; AOB87778; BCP02835; BDBM50437353; MFCD18385011; NSC758005; NSC800876; s2192; ZINC34587071; AKOS025404911; BCP9000357; CCG-264744; CS-3951; DB12183; NSC-758005; NSC-800876; QC-7257; SB16597; NCGC00346573-01; NCGC00346573-05; AC-32815; AS-17066; HY-13050; SMR004703033; FT-0700374; SW219260-1; J-513371; Q27088689; 2-(4-(4-(3-chloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-N-methylacetamide; 2-(4-{[4-(3-chloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxy}piperidin-1-yl)-N-methylacetamide; 2-[4-[4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]-N-methylacetamide
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Indication
In total 1 Indication(s)
Breast cancer [ICD-11: 2C60]
Approved
[1]
Structure
Drug Resistance Disease(s)
Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
[1]
Target Erbb2 tyrosine kinase receptor (HER2) ERBB2_HUMAN [1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula
7
IsoSMILES
CNC(=O)CN1CCC(CC1)OC2=C(C=C3C(=C2)C(=NC=N3)NC4=C(C(=CC=C4)Cl)F)OC
InChI
InChI=1S/C23H25ClFN5O3/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/h3-5,10-11,13-14H,6-9,12H2,1-2H3,(H,26,31)(H,27,28,29)
InChIKey
DFJSJLGUIXFDJP-UHFFFAOYSA-N
PubChem CID
11488320
ChEBI ID
CHEBI:132986
DrugBank ID
DB12183
Type(s) of Resistant Mechanism of This Drug
  ADTT: Aberration of the Drug's Therapeutic Target
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Click to Show/Hide the Resistance Disease of This Class
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
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Drug Resistance Data Categorized by Their Corresponding Mechanisms
       Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.L869R (c.2606T>G)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.L755S (c.2263_2264delCTinsAG)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.L755P (c.2264T>C)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.D769N (c.2305G>A)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.D769H (c.2305G>C)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.D769Y (c.2305G>T)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Duplication
p.Y772_A775 (c.2314_2325)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.V773M (c.2317G>A)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Complex-indel
p.G776_776delinsLC (c.2326_2328delinsCTTTGT)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Complex-indel
p.G776_776delinsVV (c.2326_2328delinsGTAGTA)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Complex-indel
p.G776_776delinsVC (c.2326_2328delinsGTATGT)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.V777L (c.2329G>C)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Duplication
p.G778_P780 (c.2332_2340)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration IF-insertion
p.G778_S779insLPS (c.2334_2335insCTTCCTAGC)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.L786V (c.2356C>G)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.V842I (c.2524G>A)
 Molecule Info 
Resistant Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model MCF10A cells Breast Homo sapiens (Human) CVCL_0598
CW-2 cells Colon Homo sapiens (Human) CVCL_1151
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
In Vivo Model NOD.Cg-Prkdcscid IL2rtftmWjl/Szj xenograft model Mus musculus
Experiment for
Drug Resistance		 Cell Titer Glo assay
References
Ref 1 Pan-Cancer Landscape and Analysis of ERBB2 Mutations Identifies Poziotinib as a Clinically Active Inhibitor and Enhancer of T-DM1 ActivityCancer Cell. 2019 Oct 14;36(4):444-457.e7. doi: 10.1016/j.ccell.2019.09.001. Epub 2019 Oct 3.

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