Drug Information

Drug (ID: DG01599) and It's Reported Resistant Information

• Name: Altiratinib
• Synonyms: Altiratinib; 1345847-93-9; DCC-2701; DP-5164; Altiratinib [USAN]; UNII-T678746713; Altiratinib (USAN); 1,1-Cyclopropanedicarboxamide, N-[4-[[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]oxy]-2,5-difluorophenyl]-N'-(4-fluorophenyl)-; T678746713; 1,1-Cyclopropanedicarboxamide, N-(4-((2-((cyclopropylcarbonyl)amino)-4-pyridinyl)oxy)-2,5-difluorophenyl)-N'-(4-fluorophenyl)-; 1-N'-[4-[2-(cyclopropanecarbonylamino)pyridin-4-yl]oxy-2,5-difluorophenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; N-(4-((2-(cyclopropanecarboxamido)pyridin-4-yl)oxy)-2,5-difluorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.; N-[4-[[2-[(Cyclopropylcarbonyl)amino]-4-pyridinyl]oxy]-2,5-difluorophenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide; Altiratinib;DCC2701; Altiratinib(DCC-2701); SCHEMBL139906; GTPL9174; CHEMBL3545365; DCC-270; DCC2701; EX-A902; AOB87118; BCP15682; HY-B0791; BDBM50193395; MFCD28900672; NSC784590; s6412; AKOS026750329; ZINC113198271; CS-3944; NSC-784590; SB18876; NCGC00480913-04; N-(4-((2-((Cyclopropylcarbonyl)amino)pyridin-4-yl)oxy)-2,5-difluorophenyi)-N-(4- fluorophenyl)cyclopropane-1,1-dicarboxamide; B5832; FT-0700171; A14387; D10862; F11464; A887875; J-690136; Q27074416; 1,1-CYCLOPROPANEDICARBOXAMIDE, N-[4-[[2-[(CYCLOPROPYLCARBONYL)AMINO]-4-PYRIDINYL]OXY]-2,5-DIFLUOROPHENYL]-N-(4-FLUOROPHENYL)-; 4-{5-[(E)-2-{4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl}vinyl]-1,3,4-oxadiazol-2-yl}benzonitrile; N-(4-(2-(cyclopropanecarboxamido)pyridin-4-yloxy)-2,5-difluorophenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
• Indication:
  In total 2 Indication(s)
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Phase 1; [1]
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Investigative; [1]
• Target: Vascular endothelial growth factor receptor 2 (KDR); VGFR2_HUMAN; [1]
• Formula: 8
• IsoSMILES: C1CC1C(=O)NC2=NC=CC(=C2)OC3=C(C=C(C(=C3)F)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F)F
• InChI: InChI=1S/C26H21F3N4O4/c27-15-3-5-16(6-4-15)31-24(35)26(8-9-26)25(36)32-20-12-19(29)21(13-18(20)28)37-17-7-10-30-22(11-17)33-23(34)14-1-2-14/h3-7,10-14H,1-2,8-9H2,(H,31,35)(H,32,36)(H,30,33,34)
• InChIKey: GNNDEPIMDAZHRQ-UHFFFAOYSA-N
• PubChem CID: 54576299

Type(s) of Resistant Mechanism of This Drug

  RTDM: Regulation by the Disease Microenvironment

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Regulation by the Disease Microenvironment (RTDM)

Key Molecule: Hepatocyte growth factor receptor (MET) [1]

• Molecule Alteration: Missense mutation; p.D1228N (c.3682G>A)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A549 cells; Lung; Homo sapiens (Human); CVCL_0023
• In Vitro Model: A375 cells; Skin; Homo sapiens (Human); CVCL_0132
• In Vitro Model: THP-1 cells; Blood; Homo sapiens (Human); CVCL_0006
• In Vitro Model: K562 cells; Blood; Homo sapiens (Human); CVCL_0004
• In Vitro Model: MkN-45 cells; Gastric; Homo sapiens (Human); CVCL_0434
• In Vitro Model: Sk-N-SH cells; Adrenal; Homo sapiens (Human); CVCL_0531
• In Vitro Model: HCT-116 cells; Colon; Homo sapiens (Human); N.A.
• In Vitro Model: EBC-1 cells; Lung; Homo sapiens (Human); CVCL_2891
• In Vitro Model: MRC-5 cells; Lung; Homo sapiens (Human); CVCL_0440
• In Vitro Model: PC-3 cells; Prostate; Homo sapiens (Human); CVCL_0035
• In Vitro Model: HUVEC cells; Endothelium; Homo sapiens (Human); N.A.
• In Vitro Model: HUVEC cells; Endothelium; Homo sapiens (Human); N.A.
• In Vitro Model: U87-MG cells; Brain; Homo sapiens (Human); CVCL_0022
• In Vitro Model: SkMEL5 cells; Skin; Homo sapiens (Human); CVCL_0527
• In Vitro Model: SkMEL28 cells; Skin; Homo sapiens (Human); CVCL_0526
• In Vitro Model: MV-4-11 cells; Peripheral blood; Homo sapiens (Human); CVCL_0064
• In Vitro Model: M-NFS-60 cells; Blood; Mus musculus (Mouse); CVCL_3543
• In Vitro Model: KM-12 cells; Colon; Homo sapiens (Human); CVCL_1331
• In Vitro Model: HMVEC cells; Blood vessel; Homo sapiens (Human); N.A.
• In Vitro Model: EAhy926 cells; N.A.; Homo sapiens (Human); CVCL_3901
• In Vitro Model: CHO-K cells; Ovary; Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus); CVCL_0213
• In Vitro Model: BT-474 cells; Breast; Homo sapiens (Human); CVCL_0179
• In Vitro Model: B16/F10 cells; Skin; Mus musculus (Mouse); CVCL_0159
• In Vivo Model: Mouse xenograft efficacy model; MKN-45 xenograft mouse pharmacokinetic/pharmacodynamic model; Orthotopic U87-MG xenograft efficacy model; Orthotopic U87-MG xenograft survival model; PyMT syngeneic breast cancer model; Mus musculus
• Experiment for Molecule Alteration: Enzyme-linked immunosorbent assay; Western blotting analysis
• Experiment for Drug Resistance: Resazurin cell viability assay

Key Molecule: Hepatocyte growth factor receptor (MET) [1]

• Molecule Alteration: Missense mutation; p.Y1230H (c.3688T>C)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A549 cells; Lung; Homo sapiens (Human); CVCL_0023
• In Vitro Model: A375 cells; Skin; Homo sapiens (Human); CVCL_0132
• In Vitro Model: THP-1 cells; Blood; Homo sapiens (Human); CVCL_0006
• In Vitro Model: K562 cells; Blood; Homo sapiens (Human); CVCL_0004
• In Vitro Model: MkN-45 cells; Gastric; Homo sapiens (Human); CVCL_0434
• In Vitro Model: Sk-N-SH cells; Adrenal; Homo sapiens (Human); CVCL_0531
• In Vitro Model: HCT-116 cells; Colon; Homo sapiens (Human); N.A.
• In Vitro Model: EBC-1 cells; Lung; Homo sapiens (Human); CVCL_2891
• In Vitro Model: MRC-5 cells; Lung; Homo sapiens (Human); CVCL_0440
• In Vitro Model: PC-3 cells; Prostate; Homo sapiens (Human); CVCL_0035
• In Vitro Model: HUVEC cells; Endothelium; Homo sapiens (Human); N.A.
• In Vitro Model: HUVEC cells; Endothelium; Homo sapiens (Human); N.A.
• In Vitro Model: U87-MG cells; Brain; Homo sapiens (Human); CVCL_0022
• In Vitro Model: SkMEL5 cells; Skin; Homo sapiens (Human); CVCL_0527
• In Vitro Model: SkMEL28 cells; Skin; Homo sapiens (Human); CVCL_0526
• In Vitro Model: MV-4-11 cells; Peripheral blood; Homo sapiens (Human); CVCL_0064
• In Vitro Model: M-NFS-60 cells; Blood; Mus musculus (Mouse); CVCL_3543
• In Vitro Model: KM-12 cells; Colon; Homo sapiens (Human); CVCL_1331
• In Vitro Model: HMVEC cells; Blood vessel; Homo sapiens (Human); N.A.
• In Vitro Model: EAhy926 cells; N.A.; Homo sapiens (Human); CVCL_3901
• In Vitro Model: CHO-K cells; Ovary; Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus); CVCL_0213
• In Vitro Model: BT-474 cells; Breast; Homo sapiens (Human); CVCL_0179
• In Vitro Model: B16/F10 cells; Skin; Mus musculus (Mouse); CVCL_0159
• In Vivo Model: Mouse xenograft efficacy model; MKN-45 xenograft mouse pharmacokinetic/pharmacodynamic model; Orthotopic U87-MG xenograft efficacy model; Orthotopic U87-MG xenograft survival model; PyMT syngeneic breast cancer model; Mus musculus
• Experiment for Molecule Alteration: Enzyme-linked immunosorbent assay; Western blotting analysis
• Experiment for Drug Resistance: Resazurin cell viability assay

Key Molecule: Hepatocyte growth factor receptor (MET) [1]

• Molecule Alteration: Missense mutation; p.Y1230D (c.3688T>G)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A549 cells; Lung; Homo sapiens (Human); CVCL_0023
• In Vitro Model: A375 cells; Skin; Homo sapiens (Human); CVCL_0132
• In Vitro Model: THP-1 cells; Blood; Homo sapiens (Human); CVCL_0006
• In Vitro Model: K562 cells; Blood; Homo sapiens (Human); CVCL_0004
• In Vitro Model: MkN-45 cells; Gastric; Homo sapiens (Human); CVCL_0434
• In Vitro Model: Sk-N-SH cells; Adrenal; Homo sapiens (Human); CVCL_0531
• In Vitro Model: HCT-116 cells; Colon; Homo sapiens (Human); N.A.
• In Vitro Model: EBC-1 cells; Lung; Homo sapiens (Human); CVCL_2891
• In Vitro Model: MRC-5 cells; Lung; Homo sapiens (Human); CVCL_0440
• In Vitro Model: PC-3 cells; Prostate; Homo sapiens (Human); CVCL_0035
• In Vitro Model: HUVEC cells; Endothelium; Homo sapiens (Human); N.A.
• In Vitro Model: HUVEC cells; Endothelium; Homo sapiens (Human); N.A.
• In Vitro Model: U87-MG cells; Brain; Homo sapiens (Human); CVCL_0022
• In Vitro Model: SkMEL5 cells; Skin; Homo sapiens (Human); CVCL_0527
• In Vitro Model: SkMEL28 cells; Skin; Homo sapiens (Human); CVCL_0526
• In Vitro Model: MV-4-11 cells; Peripheral blood; Homo sapiens (Human); CVCL_0064
• In Vitro Model: M-NFS-60 cells; Blood; Mus musculus (Mouse); CVCL_3543
• In Vitro Model: KM-12 cells; Colon; Homo sapiens (Human); CVCL_1331
• In Vitro Model: HMVEC cells; Blood vessel; Homo sapiens (Human); N.A.
• In Vitro Model: EAhy926 cells; N.A.; Homo sapiens (Human); CVCL_3901
• In Vitro Model: CHO-K cells; Ovary; Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus); CVCL_0213
• In Vitro Model: BT-474 cells; Breast; Homo sapiens (Human); CVCL_0179
• In Vitro Model: B16/F10 cells; Skin; Mus musculus (Mouse); CVCL_0159
• In Vivo Model: Mouse xenograft efficacy model; MKN-45 xenograft mouse pharmacokinetic/pharmacodynamic model; Orthotopic U87-MG xenograft efficacy model; Orthotopic U87-MG xenograft survival model; PyMT syngeneic breast cancer model; Mus musculus
• Experiment for Molecule Alteration: Enzyme-linked immunosorbent assay; Western blotting analysis
• Experiment for Drug Resistance: Resazurin cell viability assay

Key Molecule: Hepatocyte growth factor receptor (MET) [1]

• Molecule Alteration: Missense mutation; p.Y1230C (c.3689A>G)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A549 cells; Lung; Homo sapiens (Human); CVCL_0023
• In Vitro Model: A375 cells; Skin; Homo sapiens (Human); CVCL_0132
• In Vitro Model: THP-1 cells; Blood; Homo sapiens (Human); CVCL_0006
• In Vitro Model: K562 cells; Blood; Homo sapiens (Human); CVCL_0004
• In Vitro Model: MkN-45 cells; Gastric; Homo sapiens (Human); CVCL_0434
• In Vitro Model: Sk-N-SH cells; Adrenal; Homo sapiens (Human); CVCL_0531
• In Vitro Model: HCT-116 cells; Colon; Homo sapiens (Human); N.A.
• In Vitro Model: EBC-1 cells; Lung; Homo sapiens (Human); CVCL_2891
• In Vitro Model: MRC-5 cells; Lung; Homo sapiens (Human); CVCL_0440
• In Vitro Model: PC-3 cells; Prostate; Homo sapiens (Human); CVCL_0035
• In Vitro Model: HUVEC cells; Endothelium; Homo sapiens (Human); N.A.
• In Vitro Model: HUVEC cells; Endothelium; Homo sapiens (Human); N.A.
• In Vitro Model: U87-MG cells; Brain; Homo sapiens (Human); CVCL_0022
• In Vitro Model: SkMEL5 cells; Skin; Homo sapiens (Human); CVCL_0527
• In Vitro Model: SkMEL28 cells; Skin; Homo sapiens (Human); CVCL_0526
• In Vitro Model: MV-4-11 cells; Peripheral blood; Homo sapiens (Human); CVCL_0064
• In Vitro Model: M-NFS-60 cells; Blood; Mus musculus (Mouse); CVCL_3543
• In Vitro Model: KM-12 cells; Colon; Homo sapiens (Human); CVCL_1331
• In Vitro Model: HMVEC cells; Blood vessel; Homo sapiens (Human); N.A.
• In Vitro Model: EAhy926 cells; N.A.; Homo sapiens (Human); CVCL_3901
• In Vitro Model: CHO-K cells; Ovary; Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus); CVCL_0213
• In Vitro Model: BT-474 cells; Breast; Homo sapiens (Human); CVCL_0179
• In Vitro Model: B16/F10 cells; Skin; Mus musculus (Mouse); CVCL_0159
• In Vivo Model: Mouse xenograft efficacy model; MKN-45 xenograft mouse pharmacokinetic/pharmacodynamic model; Orthotopic U87-MG xenograft efficacy model; Orthotopic U87-MG xenograft survival model; PyMT syngeneic breast cancer model; Mus musculus
• Experiment for Molecule Alteration: Enzyme-linked immunosorbent assay; Western blotting analysis
• Experiment for Drug Resistance: Resazurin cell viability assay

Key Molecule: Hepatocyte growth factor receptor (MET) [1]

• Molecule Alteration: Missense mutation; p.M1250T (c.3749T>C)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A549 cells; Lung; Homo sapiens (Human); CVCL_0023
• In Vitro Model: A375 cells; Skin; Homo sapiens (Human); CVCL_0132
• In Vitro Model: THP-1 cells; Blood; Homo sapiens (Human); CVCL_0006
• In Vitro Model: K562 cells; Blood; Homo sapiens (Human); CVCL_0004
• In Vitro Model: MkN-45 cells; Gastric; Homo sapiens (Human); CVCL_0434
• In Vitro Model: Sk-N-SH cells; Adrenal; Homo sapiens (Human); CVCL_0531
• In Vitro Model: HCT-116 cells; Colon; Homo sapiens (Human); N.A.
• In Vitro Model: EBC-1 cells; Lung; Homo sapiens (Human); CVCL_2891
• In Vitro Model: MRC-5 cells; Lung; Homo sapiens (Human); CVCL_0440
• In Vitro Model: PC-3 cells; Prostate; Homo sapiens (Human); CVCL_0035
• In Vitro Model: HUVEC cells; Endothelium; Homo sapiens (Human); N.A.
• In Vitro Model: HUVEC cells; Endothelium; Homo sapiens (Human); N.A.
• In Vitro Model: U87-MG cells; Brain; Homo sapiens (Human); CVCL_0022
• In Vitro Model: SkMEL5 cells; Skin; Homo sapiens (Human); CVCL_0527
• In Vitro Model: SkMEL28 cells; Skin; Homo sapiens (Human); CVCL_0526
• In Vitro Model: MV-4-11 cells; Peripheral blood; Homo sapiens (Human); CVCL_0064
• In Vitro Model: M-NFS-60 cells; Blood; Mus musculus (Mouse); CVCL_3543
• In Vitro Model: KM-12 cells; Colon; Homo sapiens (Human); CVCL_1331
• In Vitro Model: HMVEC cells; Blood vessel; Homo sapiens (Human); N.A.
• In Vitro Model: EAhy926 cells; N.A.; Homo sapiens (Human); CVCL_3901
• In Vitro Model: CHO-K cells; Ovary; Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus); CVCL_0213
• In Vitro Model: BT-474 cells; Breast; Homo sapiens (Human); CVCL_0179
• In Vitro Model: B16/F10 cells; Skin; Mus musculus (Mouse); CVCL_0159
• In Vivo Model: Mouse xenograft efficacy model; MKN-45 xenograft mouse pharmacokinetic/pharmacodynamic model; Orthotopic U87-MG xenograft efficacy model; Orthotopic U87-MG xenograft survival model; PyMT syngeneic breast cancer model; Mus musculus
• Experiment for Molecule Alteration: Enzyme-linked immunosorbent assay; Western blotting analysis
• Experiment for Drug Resistance: Resazurin cell viability assay

References

• Ref 1: Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2Mol Cancer Ther. 2015 Sep;14(9):2023-34. doi: 10.1158/1535-7163.MCT-14-1105. Epub 2015 Aug 18.