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 |
|---|---|
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 |
(Kd <100 nM)