Linsitinib - Small Molecule (ID:10135-101)
| HMS LINCS ID: |
10135-101
|
| Name: | Linsitinib |
| Alternative Names: | OSI 906 |
| LINCS ID: | LSM-1135 |
| PubChem CID: | 11640390 |
| ChEBI ID: | |
| ChEMBL ID: | 1091644 |
| Molecular Mass: | 421.19 |
| InChi: | InChI=1S/C26H23N5O/c1-26(32)14-19(15-26)25-30-22(23-24(27)28-11-12-31(23)25)18-8-7-17-9-10-20(29-21(17)13-18)16-5-3-2-4-6-16/h2-13,19,32H,14-15H2,1H3,(H2,27,28) |
| InChi Key: | PKCDDUHJAFVJJB-UHFFFAOYSA-N |
| SMILES: | CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O |
| Relevant Citations: | |
| Comments: | |
| Date Publicly Available: | |
| Most Recent Update: | 2016-04-04 |
Target Affinity:
(see Study 20000)| Target Affinity Spectrum Value | HUGO Gene Name |
|---|---|
IGF1R, INSR | |
2 (equivalent to 100 nM ≤ Kd < 1µM) | ABL1, AIM1, AURKB, BLK, ERBB4, FLT1, FLT4, FYN, LCK, LYN, MAP4K2, MAP4K5, RET, ROCK1 |
3 (equivalent to 1µM ≤ Kd < 10 µM) | AKT1, AKT2, ALK, AURKA, BTK, CAMK1, CAMK2B, CAMK2D, CAMK2G, CDC42BPA, CDC7, CDK1, CDK2, CHEK1, CHEK2, CLK2, CSF1R, CSNK1A1, CSNK1D, CSNK1G1, CSNK1G2, CSNK1G3, CSNK2A1, DAPK3, DYRK1A, DYRK4, EGFR, EPHA2, ERBB2, FER, FES, FGFR1, FGFR3, FLG, FLT3, FRK, GSK3A, GSK3B, HIPK2, HIPK4, IRAK1, ITK, JAK2, JAK3, KDR, KIT, MAPK1, MAPK12, MAPK13, MAPK8, MAPK9, MAPKAPK2, MAPKAPK5, MARK2, MARK3, MATK, MELK, MET, NEK2, NEK4, NTRK1, NTRK2, NTRK3, PAK4, PDK1, PDPK1, PHKG2, PIM2, PIM3, PKN2, PLK1, PLK3, PLK4, PRKAA1, PRKACA, PRKCD, PRKCG, PRKCI, PRKCZ, PRKG1, PRKG2, PRKX, ROCK2, ROS1, RPS6KA3, RPS6KA5, RPS6KB1, SRC, SRMS, SRPK1, STK17A, STK3, SYK, TSSK1B, TSSK2, TYK2, TYRO3 |
10 (confirmed non-binding) |
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 |
| 20256 | Breast Cancer Cell Density: Imaging assay of the density- and context-dependence of small molecule perturbagen response in breast cancer cell lines. Dataset 1 of 3: Cell count and normalized growth rate inhibition values. | Microscopy/Imaging |
| 20257 | Breast Cancer Cell Density: Imaging assay of the density- and context-dependence of small molecule perturbagen response in breast cancer cell lines. Dataset 2 of 3: Mean cell count and mean normalized growth rate inhibition values across all replicates. | Microscopy/Imaging |
| 20258 | Breast Cancer Cell Density: Imaging assay of the density- and context-dependence of small molecule perturbagen response in breast cancer cell lines. Dataset 3 of 3: Calculated dose-response metrics. | Analysis |
Batch Information:
| HMS LINCS Batch ID | Provider | Provider Batch ID |
|---|---|---|
| 10135-101-1 | Haoyuan chemexpress | HM-101_17-20110627 |
| 10135-101-2 | Selleck Chemicals | |
| 10135-101-3 | MedChem Express | 09453 |
(Kd <100 nM)