Drug (ID: DG01567) and It's Reported Resistant Information
Name
Pimasertib
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)
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Phase 2
[1]
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Phase 2
[1]
Structure
Target MAPK/ERK kinase kinase (MAP3K) NOUNIPROTAC [1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula
6
IsoSMILES
C1=CC(=C(C=C1I)F)NC2=C(C=CN=C2)C(=O)NC[C@@H](CO)O
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
InChIKey
VIUAUNHCRHHYNE-JTQLQIEISA-N
PubChem CID
44187362
ChEBI ID
CHEBI:94793
TTD Drug ID
D03SKL
VARIDT ID
DR1835
DrugBank ID
DB14904
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
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Colorectal cancer [ICD-11: 2B91]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) [1]
Molecule Alteration Missense mutation
p.V600E (c.1799T>A)
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
Ref 1 Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cellsInt J Cancer. 2013 Nov;133(9):2089-101. doi: 10.1002/ijc.28236. Epub 2013 May 29.

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