Drug Information
Drug (ID: DG01567) and It's Reported Resistant Information
Name |
Pimasertib
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Synonyms |
Pimasertib; 1236699-92-5; AS703026; AS-703026; Pimasertib (AS-703026); MSC1936369B; AS 703026; UNII-6ON9RK82AL; 1204531-26-9; 6ON9RK82AL; SAR 245509; MSC-1936369; N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodo-anilino)pyridine-4-carboxamide; N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]pyridine-4-carboxamide; C15H15FIN3O3; (S)-N-(2,3-dihydroxypropyl)-3-(2-fluoro-4-iodophenylamino)isonicotinamide; (S)-N-(2,3-dihydroxypropyl)-3-((2-fluoro-4-iodophenyl)amino)isonicotinamide; (S)-N-(2,3-dihydroxypropyl)-3-((2-fluoro-4-iodophenyl)amino)isonicotinamide.; 4-Pyridinecarboxamide, N-((2S)-2,3-dihydroxypropyl)-3-((2-fluoro-4-iodophenyl)amino)-; 4-Pyridinecarboxamide, N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]-; N-((2S)-2,3-dihydroxypropyl)-3-((2-fluoro-4-iodophenyl)amino)pyridine-4-carboxamide; N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)pyridine-4-carboxamide; Pimasertib [USAN:INN]; Pimasertib (USAN/INN); Pimasertib; AS703026; N-[(2S)-2,3-Dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]-4-pyridinecarboxamide; MLS006010177; GTPL7872; QCR-17; SCHEMBL2720659; CHEMBL2107832; CHEBI:94793; DTXSID40152870; EX-A403; SYN1190; BCPP000386; AOB87391; BCP02094; MSC1936369A; BDBM50014412; MSC-1936369A; NSC755763; NSC800854; ZINC38226009; AKOS022186348; BCP9000325; CCG-269018; CS-0198; DB14904; NSC-755763; NSC-800854; EMD 1036239; EMD-1036239; NCGC00346530-01; AC-32862; AS-16324; HY-12042; SMR004701285; AS703026,MSC1936369B; SW219691-1; X7392; C71933; D10426; A857420; J-523298; BRD-K89014967-001-01-9; Q27088393; G-02443714; AS7030261236699-92-5; AS-703026;N-[(2S)-2,3-Dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]-4-pyridinecarboxamide;AS-703026
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Indication |
In total 2 Indication(s)
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Structure | |||||
Target | MAPK/ERK kinase kinase (MAP3K) | NOUNIPROTAC | [1] | ||
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Formula |
6
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IsoSMILES |
C1=CC(=C(C=C1I)F)NC2=C(C=CN=C2)C(=O)NC[C@@H](CO)O
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InChI |
InChI=1S/C15H15FIN3O3/c16-12-5-9(17)1-2-13(12)20-14-7-18-4-3-11(14)15(23)19-6-10(22)8-21/h1-5,7,10,20-22H,6,8H2,(H,19,23)/t10-/m0/s1
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InChIKey |
VIUAUNHCRHHYNE-JTQLQIEISA-N
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PubChem CID | |||||
ChEBI ID | |||||
TTD Drug ID | |||||
VARIDT ID | |||||
DrugBank ID |
Type(s) of Resistant Mechanism of This Drug
UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Colorectal cancer [ICD-11: 2B91]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [1] | |||
Molecule Alteration | Missense mutation | p.V600E (c.1799T>A) |
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Sensitive Disease | Colorectal cancer [ICD-11: 2B91.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HT29 Cells | Colon | Homo sapiens (Human) | CVCL_A8EZ |
H1975 cells | Lung | Homo sapiens (Human) | CVCL_1511 | |
A549 cells | Lung | Homo sapiens (Human) | CVCL_0023 | |
H460 cells | Lung | Homo sapiens (Human) | CVCL_0459 | |
LOVO cells | Colon | Homo sapiens (Human) | CVCL_0399 | |
H1299 cells | Lung | Homo sapiens (Human) | CVCL_0060 | |
HCT15 cells | Colon | Homo sapiens (Human) | CVCL_0292 | |
COLO205 cells | Colon | Homo sapiens (Human) | CVCL_F402 | |
In Vivo Model | Female balb/c athymic (nu+/nu+) mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Immunoblotting analysis | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | The missense mutation p.V600E (c.1799T>A) in gene BRAF cause the sensitivity of Pimasertib by aberration of the drug's therapeutic target |
References
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