Drug Information
Drug (ID: DG01577) and It's Reported Resistant Information
Name |
Flumatinib
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Synonyms |
Flumatinib; 895519-90-1; HHGV678; HH-GV678; Flumatinib free base; flumbatinib; UNII-R4009Y24AI; HHGV-678; R4009Y24AI; 895519-90-1 (free base); 4-[(4-methylpiperazin-1-yl)methyl]-N-[6-methyl-5-[(4-pyridin-3-ylpyrimidin-2-yl)amino]pyridin-3-yl]-3-(trifluoromethyl)benzamide; HHGV678 mesylate; BenzaMide, 4-[(4-Methyl-1-piperazinyl)Methyl]-N-[6-Methyl-5-[[4-(3-pyridinyl)-2-pyriMidinyl]aMino]-3-pyridinyl]-3-(trifluoroMethyl)-; N-(6-methyl-5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)pyridin-3-yl)-4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)benzamide; HH-GV-678; Hansoh Xinfu; flumatinib (pseudo INN); GTPL9913; SCHEMBL4883843; CHEMBL3545413; DTXSID60237779; BCP23797; EX-A3572; VKB51990; BDBM50529313; NSC830368; ZINC68244727; CS-5550; DB11904; NSC-830368; SB17192; NCGC00378614-01; 4-(4-Methylpiperazin-1-ylmethyl)-N-(6-methyl-5-(4-pyridin-3-ylpyrimidin-2-ylamino)pyridin-3-yl)-3-trifluoromethylbenzamide; DA-33625; HY-13904; FT-0739882; Q27287759; N-[5-[[4-(3-Pyridinyl)pyrimidine-2-yl]amino]-6-methylpyridine-3-yl]-3-(trifluoromethyl)-4-[(4-methylpiperazine-1-yl)methyl]benzamide
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Indication |
In total 3 Indication(s)
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Structure | |||||
Drug Resistance Disease(s) |
Disease(s) with Clinically Reported Resistance for This Drug
(1 diseases)
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
[1]
Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug
(1 diseases)
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
[1]
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Target | RAC-alpha serine/threonine-protein kinase (AKT1) | AKT1_HUMAN | [1] | ||
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Formula |
7
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IsoSMILES |
CC1=C(C=C(C=N1)NC(=O)C2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CC=C5
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InChI |
InChI=1S/C29H29F3N8O/c1-19-26(38-28-34-9-7-25(37-28)21-4-3-8-33-16-21)15-23(17-35-19)36-27(41)20-5-6-22(24(14-20)29(30,31)32)18-40-12-10-39(2)11-13-40/h3-9,14-17H,10-13,18H2,1-2H3,(H,36,41)(H,34,37,38)
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InChIKey |
BJCJYEYYYGBROF-UHFFFAOYSA-N
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PubChem CID | |||||
TTD Drug ID | |||||
DrugBank ID |
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 Resistance Data Categorized by Their Corresponding Mechanisms | ||||
Aberration of the Drug's Therapeutic Target (ADTT) | ||||
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) | [1] | |||
Molecule Alteration | Duplication | p.I571_D579 (c.1711_1737) |
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Resistant Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | 32D cells | Bone marrow | Homo sapiens (Human) | CVCL_0118 |
In Vivo Model | Female Balb/cA-nu/nu mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | The duplication p.I571_D579 (c.1711_1737) in gene KIT cause the resistance of Flumatinib by aberration of the drug's therapeutic target. | |||
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) | [1] | |||
Molecule Alteration | Missense mutation | p.D816Y (c.2446G>T) |
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Resistant Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | IL-3-dependent murine hematopoietic cells | Blood | Mus musculus (Mouse) | CVCL_2015 |
IL-3-dependent murine hematopoietic cells | Blood | Mus musculus (Mouse) | CVCL_2015 | |
In Vivo Model | Female Balb/cA-nu/nu mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
MTT assay | |||
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) | [1] | |||
Molecule Alteration | Missense mutation | p.D816V (c.2447A>T) |
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Resistant Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | IL-3-dependent murine hematopoietic cells | Blood | Mus musculus (Mouse) | CVCL_2015 |
IL-3-dependent murine hematopoietic cells | Blood | Mus musculus (Mouse) | CVCL_2015 | |
In Vivo Model | Female Balb/cA-nu/nu mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
MTT assay |
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Aberration of the Drug's Therapeutic Target (ADTT) | ||||
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) | [1] | |||
Molecule Alteration | Complex-indel | p.T417_D419delinsI (c.1249_1257delinsATC) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | 32D cells | Bone marrow | Homo sapiens (Human) | CVCL_0118 |
In Vivo Model | Female Balb/cA-nu/nu mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | The complex-indel p.T417_D419delinsI (c.1249_1257delinsATC) in gene KIT cause the sensitivity of Flumatinib by aberration of the drug's therapeutic target. | |||
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) | [1] | |||
Molecule Alteration | Duplication | p.A502_Y503 (c.1504_1509) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | 32D cells | Bone marrow | Homo sapiens (Human) | CVCL_0118 |
In Vivo Model | Female Balb/cA-nu/nu mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | The duplication p.A502_Y503 (c.1504_1509) in gene KIT cause the sensitivity of Flumatinib by aberration of the drug's therapeutic target. | |||
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) | [1] | |||
Molecule Alteration | IF-deletion | p.V559_V560delVV (c.1676_1681delTTGTTG) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | 32D cells | Bone marrow | Homo sapiens (Human) | CVCL_0118 |
In Vivo Model | Female Balb/cA-nu/nu mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | The if-deletion p.V559_V560delVV (c.1676_1681delTTGTTG) in gene KIT cause the sensitivity of Flumatinib by aberration of the drug's therapeutic target. | |||
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) | [1] | |||
Molecule Alteration | Missense mutation | p.N822K (c.2466T>G) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | 32D cells | Bone marrow | Homo sapiens (Human) | CVCL_0118 |
In Vivo Model | Female Balb/cA-nu/nu mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | The missense mutation p.N822K (c.2466T>G) in gene KIT cause the sensitivity of Flumatinib by aberration of the drug's therapeutic target | |||
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) | [1] | |||
Molecule Alteration | Missense mutation | p.V559D (c.1676T>A) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | 32D cells | Bone marrow | Homo sapiens (Human) | CVCL_0118 |
In Vivo Model | Female Balb/cA-nu/nu mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | The missense mutation p.V559D (c.1676T>A) in gene KIT cause the sensitivity of Flumatinib by aberration of the drug's therapeutic target | |||
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) | [1] | |||
Molecule Alteration | Missense mutation | p.D816H (c.2446G>C) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | 32D cells | Bone marrow | Homo sapiens (Human) | CVCL_0118 |
In Vivo Model | Female Balb/cA-nu/nu mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | The missense mutation p.D816H (c.2446G>C) in gene KIT cause the sensitivity of Flumatinib by aberration of the drug's therapeutic target |
References
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