Drug Information

Drug (ID: DG01560) and It's Reported Resistant Information

• Name: ALW-II-41-27
• Synonyms: ALW-II-41-27; 1186206-79-0; N-(5-((4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)-2-methylphenyl)-5-(thiophen-2-yl)nicotinamide; ALW II-41-27; Benzamide, N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-[[[5-(2-thienyl)-3-pyridinyl]carbonyl]amino]-; N-[5-[[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]carbamoyl]-2-methylphenyl]-5-thiophen-2-ylpyridine-3-carboxamide; MLS002232274; CHEMBL556140; SCHEMBL20136698; DTXSID80655254; BDBM163701; HMS2043H01; HMS2218G07; HMS3333E20; BCP26205; EX-A2618; s6515; ZINC42966573; Eph receptor tyrosine kinase inhibitor; CS-1203; NCGC00390558-01; AS-78559; BA164807; HY-18007; SMR001307828; A907856; N-[5-({4-[(4-Ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}carbamoyl)-2-methylphenyl]-5-(thiophen-2-yl)pyridine-3-carboxamide; N-[5-({4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}carbamoyl)-2-methylphenyl]-5-(thiophen-2-yl)pyridine-3-carboxamide (6)
• Target: .; NOUNIPROTAC; [1]
• Formula: 8
• IsoSMILES: CCN1CCN(CC1)CC2=C(C=C(C=C2)NC(=O)C3=CC(=C(C=C3)C)NC(=O)C4=CN=CC(=C4)C5=CC=CS5)C(F)(F)F
• InChI: InChI=1S/C32H32F3N5O2S/c1-3-39-10-12-40(13-11-39)20-23-8-9-26(17-27(23)32(33,34)35)37-30(41)22-7-6-21(2)28(16-22)38-31(42)25-15-24(18-36-19-25)29-5-4-14-43-29/h4-9,14-19H,3,10-13,20H2,1-2H3,(H,37,41)(H,38,42)
• InChIKey: HYWXBDQAYLPMIX-UHFFFAOYSA-N
• PubChem CID: 42628503

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

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

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Proto-oncogene tyrosine-protein kinase receptor Ret (RET) [1]

• Molecule Alteration: Missense mutation; p.C634Y (c.1901G>A)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: TT cells; Thyroid gland; Homo sapiens (Human); CVCL_1774
• In Vitro Model: RET/V804M cells; Bone marrow; Mus musculus (Mouse); CVCL_XZ26
• In Vitro Model: RET/V804L cells; N.A.; Mus musculus (Mouse); CVCL_XZ25
• In Vitro Model: RET/S891A cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/M918T cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/M918T cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/L790F cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/E768D cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/C634R cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/C634R cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/A883F cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: MZ-CRC-1 cells; Pleural effusion; Homo sapiens (Human); CVCL_A656
• In Vitro Model: RET/V804M cells; Bone marrow; Mus musculus (Mouse); CVCL_XZ26
• In Vitro Model: RET/E768D cells; N.A.; Homo sapiens (Human); N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: Cell counting assay

Key Molecule: Proto-oncogene tyrosine-protein kinase receptor Ret (RET) [1]

• Molecule Alteration: Missense mutation; p.M918T (c.2753T>C)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: TT cells; Thyroid gland; Homo sapiens (Human); CVCL_1774
• In Vitro Model: RET/V804M cells; Bone marrow; Mus musculus (Mouse); CVCL_XZ26
• In Vitro Model: RET/V804L cells; N.A.; Mus musculus (Mouse); CVCL_XZ25
• In Vitro Model: RET/S891A cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/M918T cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/M918T cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/L790F cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/E768D cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/C634R cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/C634R cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/A883F cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: MZ-CRC-1 cells; Pleural effusion; Homo sapiens (Human); CVCL_A656
• In Vitro Model: RET/V804M cells; Bone marrow; Mus musculus (Mouse); CVCL_XZ26
• In Vitro Model: RET/E768D cells; N.A.; Homo sapiens (Human); N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: Cell counting assay

Thyroid cancer [ICD-11: 2D10]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Proto-oncogene tyrosine-protein kinase receptor Ret (RET) [1]

• Molecule Alteration: Missense mutation; p.M918T (c.2753T>C)
• Sensitive Disease: Thyroid gland cancer [ICD-11: 2D10.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: TT cells; Thyroid gland; Homo sapiens (Human); CVCL_1774
• In Vitro Model: RET/V804M cells; Bone marrow; Mus musculus (Mouse); CVCL_XZ26
• In Vitro Model: RET/V804L cells; N.A.; Mus musculus (Mouse); CVCL_XZ25
• In Vitro Model: RET/S891A cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/M918T cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/M918T cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/L790F cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/E768D cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/C634R cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/C634R cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/A883F cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: MZ-CRC-1 cells; Pleural effusion; Homo sapiens (Human); CVCL_A656
• In Vitro Model: RET/V804M cells; Bone marrow; Mus musculus (Mouse); CVCL_XZ26
• In Vitro Model: RET/E768D cells; N.A.; Homo sapiens (Human); N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: Cell counting assay

Key Molecule: Proto-oncogene tyrosine-protein kinase receptor Ret (RET) [1]

• Molecule Alteration: Missense mutation; p.C634W (c.1902C>G)
• Sensitive Disease: Thyroid gland cancer [ICD-11: 2D10.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: TT cells; Thyroid gland; Homo sapiens (Human); CVCL_1774
• In Vitro Model: RET/V804M cells; Bone marrow; Mus musculus (Mouse); CVCL_XZ26
• In Vitro Model: RET/V804L cells; N.A.; Mus musculus (Mouse); CVCL_XZ25
• In Vitro Model: RET/S891A cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/M918T cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/M918T cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/L790F cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/E768D cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/C634R cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/C634R cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: RET/A883F cells; N.A.; Homo sapiens (Human); N.A.
• In Vitro Model: MZ-CRC-1 cells; Pleural effusion; Homo sapiens (Human); CVCL_A656
• In Vitro Model: RET/V804M cells; Bone marrow; Mus musculus (Mouse); CVCL_XZ26
• In Vitro Model: RET/E768D cells; N.A.; Homo sapiens (Human); N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: Cell counting assay

References

• Ref 1: Identification of Novel Small Molecule Inhibitors of Oncogenic RET KinasePLoS One. 2015 Jun 5;10(6):e0128364. doi: 10.1371/journal.pone.0128364. eCollection 2015.