Trametinib - Small Molecule (ID:10142-101)

HMS LINCS ID: 10142-101
Name: Trametinib
Alternative Names: GSK-1120212; GSK1120212; GSK1120212B; JTP-74057
LINCS ID: LSM-1143
PubChem CID: 11707110
ChEBI ID:
ChEMBL ID:
Molecular Mass: 615.08
InChi: InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34)
InChi Key: LIRYPHYGHXZJBZ-UHFFFAOYSA-N
SMILES: CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC(=CC=C4)NC(=O)C)C5CC5
Relevant Citations:
Comments:
Date Publicly Available:
Most Recent Update: 2016-05-06

Target Affinity:

(see Study 20000)
Target Affinity Spectrum Value HUGO Gene Name
1
(Kd <100 nM)
MAP2K1, MAP2K2

Datasets:

HMS Dataset ID Dataset Title HMS Dataset Type
20000
Target Affinity Spectrum (TAS) vectors for compounds in the HMS LINCS small molecule library.
Analysis
20237
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 1 of 15: Cell count and relative growth within biological replicate 1.
Microscopy/Imaging
20238
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 2 of 15: Cell count and relative growth within biological replicate 2.
Microscopy/Imaging
20239
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 3 of 15: Cell count and relative growth within biological replicate 3.
Microscopy/Imaging
20240
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 4 of 15: Mean cell count and mean growth rate across biological replicate 1.
Microscopy/Imaging
20241
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 5 of 15: Mean cell count and mean growth rate across biological replicate 2.
Microscopy/Imaging
20242
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 6 of 15: Mean cell count and mean growth rate across biological replicate 3.
Microscopy/Imaging
20243
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 7 of 15: Mean cell count and mean growth rate across all replicates.
Microscopy/Imaging
20245
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 8 of 15: Cell count and normalized growth rate inhibition values within biological replicate 1.
Microscopy/Imaging
20246
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 9 of 15: Cell count and normalized growth rate inhibition values within biological replicate 2.
Microscopy/Imaging
20247
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 10 of 15: Cell count and normalized growth rate inhibition values within biological replicate 3.
Microscopy/Imaging
20248
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 11 of 15: Mean cell count and mean normalized growth rate inhibition values across biological replicate 1.
Microscopy/Imaging
20249
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 12 of 15: Mean cell count and mean normalized growth rate inhibition values across biological replicate 2.
Microscopy/Imaging
20250
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 13 of 15: Mean cell count and mean normalized growth rate inhibition values across biological replicate 3.
Microscopy/Imaging
20251
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 14 of 15: Mean cell count and mean normalized growth rate inhibition values across all replicates.
Microscopy/Imaging
20252
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 15 of 15: Calculated dose-response metrics.
Analysis
20259
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (drug combination treatments). Dataset 1 of 2: Cell count and normalized growth rate inhibition values.
Microscopy/Imaging
20260
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (drug combination treatments). Dataset 2 of 2: Mean cell count and mean normalized growth rate inhibition values across technical replicates.
Microscopy/Imaging
20273
Viability and apoptosis measured by imaging in BRAF(V600E/D) melanoma cell lines following treatment with combinations of three compounds (viability/apoptosis dataset 2 of 2)
Microscopy/Imaging
20274
Phosphorylation state and protein levels measured by imaging in BRAF(V600E/D) melanoma cell lines following treatment with combinations of two compounds (immunofluorescence dataset 1 of 4)
Microscopy/Imaging
20275
Phosphorylation state and protein levels measured by imaging in BRAF(V600E/D) melanoma cell lines following treatment with combinations of two compounds (immunofluorescence dataset 2 of 4)
Microscopy/Imaging
20277
Phosphorylation state and protein levels measured by imaging in BRAF(V600E/D) melanoma cell lines following treatment with combinations of two compounds (immunofluorescence dataset 4 of 4)
Microscopy/Imaging
20278
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 1 of 9: Cell count and normalized growth rate inhibition values for biological replicate 1
Microscopy/Imaging
20279
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 2 of 9: Cell count and normalized growth rate inhibition values for biological replicate 2
Microscopy/Imaging
20280
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 3 of 9: Cell count and normalized growth rate inhibition values for biological replicate 3
Microscopy/Imaging
20281
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 4 of 9: Mean cell count and mean normalized growth rate inhibition values for biological replicate 1
Microscopy/Imaging
20282
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 5 of 9: Mean cell count and mean normalized growth rate inhibition values for biological replicate 2
Microscopy/Imaging
20283
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 6 of 9: Mean cell count and mean normalized growth rate inhibition values for biological replicate 3
Microscopy/Imaging
20284
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 7 of 9: Calculated dose-response metrics for biological replicate 1
Analysis
20285
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 8 of 9: Calculated dose-response metrics for biological replicate 2
Analysis
20286
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 9 of 9: Calculated dose-response metrics for biological replicate 3
Analysis
20303
LINCS MCF 10A Common Project: Highly-multiplexed imaging by Cyclic Immunofluorescence (CycIF) of protein levels and protein phosphorylation states in the MCF 10A breast cell line treated with 8 small molecule perturbagens. Dataset 1 of 6: Cytosolic fluorescent intensity measurements at 24 hr.
Microscopy/Imaging
20304
LINCS MCF 10A Common Project: Highly-multiplexed imaging by Cyclic Immunofluorescence (CycIF) of protein levels and protein phosphorylation states in the MCF 10A breast cell line treated with 8 small molecule perturbagens. Dataset 2 of 6: Nuclear fluorescent intensity measurements at 24 hr.
Microscopy/Imaging
20305
LINCS MCF 10A Common Project: Highly-multiplexed imaging by Cyclic Immunofluorescence (CycIF) of protein levels and protein phosphorylation states in the MCF 10A breast cell line treated with 8 small molecule perturbagens. Dataset 3 of 6: Cytosolic fluorescent intensity measurements at 48 hr.
Microscopy/Imaging
20306
LINCS MCF 10A Common Project: Highly-multiplexed imaging by Cyclic Immunofluorescence (CycIF) of protein levels and protein phosphorylation states in the MCF 10A breast cell line treated with 8 small molecule perturbagens. Dataset 4 of 6: Nuclear fluorescent intensity measurements at 48 hr.
Microscopy/Imaging
20307
LINCS MCF 10A Common Project: Highly-multiplexed imaging by Cyclic Immunofluorescence (CycIF) of protein levels and protein phosphorylation states in the MCF 10A breast cell line treated with 8 small molecule perturbagens. Dataset 5 of 6: Cytosolic fluorescent intensity measurements at 72 hr.
Microscopy/Imaging
20308
LINCS MCF 10A Common Project: Highly-multiplexed imaging by Cyclic Immunofluorescence (CycIF) of protein levels and protein phosphorylation states in the MCF 10A breast cell line treated with 8 small molecule perturbagens. Dataset 6 of 6: Nuclear fluorescent intensity measurements at 72 hr.
Microscopy/Imaging
20309
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 1 of 15: End-point cell counts and normalized growth rate inhibition values for all technical replicates of biological replicate 1.
Microscopy/Imaging
20310
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 2 of 15: End-point cell counts and normalized growth rate inhibition values for all technical replicates of biological replicate 2.
Microscopy/Imaging
20311
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 3 of 15: End-point cell counts and normalized growth rate inhibition values for all technical replicates of biological replicate 3.
Microscopy/Imaging
20312
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 4 of 15: End-point mean cell counts and mean normalized growth rate inhibition values for biological replicate 1.
Microscopy/Imaging
20313
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 5 of 15: End-point mean cell counts and mean normalized growth rate inhibition values for biological replicate 2.
Microscopy/Imaging
20314
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 6 of 15: End-point mean cell counts and mean normalized growth rate inhibition values for biological replicate 3.
Microscopy/Imaging
20315
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 7 of 15: End-point dose-response metrics for biological replicate 1.
Analysis
20316
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 8 of 15: End-point dose-response metrics for biological replicate 2.
Analysis
20317
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 9 of 15: End-point dose-response metrics for biological replicate 3.
Analysis
20318
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 10 of 15: Time-dependent mean normalized growth rate inhibition values for biological replicate 1.
Microscopy/Imaging
20319
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 11 of 15: Time-dependent mean normalized growth rate inhibition values for biological replicate 2.
Microscopy/Imaging
20320
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 12 of 15: Time-dependent mean normalized growth rate inhibition values for biological replicate 3.
Microscopy/Imaging
20321
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 13 of 15: Time-dependent dose-response metrics for biological replicate 1.
Analysis
20322
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 14 of 15: Time-dependent dose-response metrics for biological replicate 2.
Analysis
20323
LINCS MCF 10A Common Project: Rolling-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Dataset 15 of 15: Time-dependent dose-response metrics for biological replicate 3.
Analysis
20343
Breast Cancer Profiling Project, Drug Sensitivity phase I: Fixed-cell GR measures of 35 breast cell lines to 34 small molecule perturbagens from library plate I. Dataset 1 of 2: Normalized growth rate inhibition values
Microscopy/Imaging
20344
Breast Cancer Profiling Project, Drug Sensitivity phase I: Fixed-cell GR measures of 35 breast cell lines to 34 small molecule perturbagens from library plate I. Dataset 2 of 2: Calculated dose response metrics
Analysis
20358
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Repeat performed by Scientist A in 2019 to assess reproducibility. Dataset 1 of 2: Normalized growth rate inhibition values.
Microscopy/Imaging
20359
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Repeat performed by Scientist B in 2019 to assess reproducibility. Dataset 1 of 2: Normalized growth rate inhibition values.
Microscopy/Imaging
20360
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Repeat performed by Scientist C to assess reproducibility. Dataset 1 of 2: Normalized growth rate inhibition values.
Microscopy/Imaging
20361
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Repeat performed by Scientist A in 2019 to assess reproducibility. Dataset 2 of 2: Calculated dose response metrics.
Analysis
20362
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Repeat performed by Scientist B in 2019 to assess reproducibility. Dataset 2 of 2: Calculated dose response metrics.
Analysis
20363
LINCS MCF 10A Common Project: Fixed-time-point sensitivity measures of the MCF 10A breast cell line to 8 small molecule perturbagens. Repeat performed by Scientist C in 2019 to assess reproducibility. Dataset 2 of 2: Calculated dose response metrics.
Analysis
20364
Evaluation of the sensitivities of six triple-negative breast cancer (TNBC) cell lines to 23 different PI3K/AKT/mTOR inhibitors or to a MEK inhibitor (trametinib). Dataset 1 of 2: GR values.
Microscopy/Imaging
20365
Evaluation of the sensitivities of six triple-negative breast cancer (TNBC) cell lines to 23 different PI3K/AKT/mTOR inhibitors or to a MEK inhibitor (trametinib). Dataset 2 of 2: GR metrics.
Analysis

Batch Information:

HMS LINCS Batch ID Provider Provider Batch ID
10142-101-1 Haoyuan chemexpress HM-078_10-20101118
10142-101-3 MedChem Express 07378
10142-101-4 MedChem Express 07378
10142-101-6 Selleck Chemicals