Lck-IN-2
Lck-IN-2 (compound 12a) is an inhibitor of Lymphocyte-specific protein tyrosine kinase (Lck) with IC50 of 10.6 nM. Lck-IN-2 reveals efficacy in colon cancer cells with GI50s of 0.24-1.26 μM. Lck-IN-2 exhibits an apoptotic effect in Colo201 cells.
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- CAS No.: 2615173-24-3
- Formule: C31H32N8O5
- Masse moléculaire:596.64
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
|
Lck 10.6 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | GI50 |
0.45 μM
Compound: 12a
|
Antiproliferative activity against human 786-0 cells
Antiproliferative activity against human 786-0 cells
|
[PMID: 38316368] |
| A498 | GI50 |
0.22 μM
Compound: 12a
|
Antiproliferative activity against human A498 cells
Antiproliferative activity against human A498 cells
|
[PMID: 38316368] |
| A549 | GI50 |
0.43 μM
Compound: 12a
|
Antiproliferative activity against human A549 cells
Antiproliferative activity against human A549 cells
|
[PMID: 38316368] |
| ACHN | GI50 |
0.15 μM
Compound: 12a
|
Antiproliferative activity against human ACHN cells
Antiproliferative activity against human ACHN cells
|
[PMID: 38316368] |
| BT-549 | GI50 |
1.37 μM
Compound: 12a
|
Antiproliferative activity against human BT-549 cells
Antiproliferative activity against human BT-549 cells
|
[PMID: 38316368] |
| CAKI-1 | GI50 |
0.06 μM
Compound: 12a
|
Antiproliferative activity against human CAKI-1 cells
Antiproliferative activity against human CAKI-1 cells
|
[PMID: 38316368] |
| COLO 201 | GI50 |
1.26 μM
Compound: 12a
|
Antiproliferative activity against human COLO201 cells
Antiproliferative activity against human COLO201 cells
|
[PMID: 38316368] |
| COLO 205 | GI50 |
0.24 μM
Compound: 12a
|
Antiproliferative activity against human COLO 205 cells
Antiproliferative activity against human COLO 205 cells
|
[PMID: 38316368] |
| DU-145 | GI50 |
0.4 μM
Compound: 12a
|
Antiproliferative activity against human DU-145 cells
Antiproliferative activity against human DU-145 cells
|
[PMID: 38316368] |
| EKVX | GI50 |
0.98 μM
Compound: 12a
|
Antiproliferative activity against human EKVX cells
Antiproliferative activity against human EKVX cells
|
[PMID: 38316368] |
| HCC 2998 | GI50 |
1.1 μM
Compound: 12a
|
Antiproliferative activity against human HCC 2998 cells
Antiproliferative activity against human HCC 2998 cells
|
[PMID: 38316368] |
| HCT-116 | GI50 |
0.33 μM
Compound: 12a
|
Antiproliferative activity against human HCT-116 cells
Antiproliferative activity against human HCT-116 cells
|
[PMID: 38316368] |
| HCT-15 | GI50 |
0.41 μM
Compound: 12a
|
Antiproliferative activity against human HCT-15 cells
Antiproliferative activity against human HCT-15 cells
|
[PMID: 38316368] |
| HL-60(TB) | GI50 |
0.23 μM
Compound: 12a
|
Antiproliferative activity against human HL-60(TB) cells
Antiproliferative activity against human HL-60(TB) cells
|
[PMID: 38316368] |
| HOP-62 | GI50 |
1.13 μM
Compound: 12a
|
Antiproliferative activity against human HOP-62 cells
Antiproliferative activity against human HOP-62 cells
|
[PMID: 38316368] |
| HOP-92 | GI50 |
0.09 μM
Compound: 12a
|
Antiproliferative activity against human HOP-92 cells
Antiproliferative activity against human HOP-92 cells
|
[PMID: 38316368] |
| Hs-578T | GI50 |
0.28 μM
Compound: 12a
|
Antiproliferative activity against human Hs-578T cells
Antiproliferative activity against human Hs-578T cells
|
[PMID: 38316368] |
| HT-29 | GI50 |
0.41 μM
Compound: 12a
|
Antiproliferative activity against human HT-29 cells
Antiproliferative activity against human HT-29 cells
|
[PMID: 38316368] |
| IGROV-1 | GI50 |
0.21 μM
Compound: 12a
|
Antiproliferative activity against human IGROV-1 cells
Antiproliferative activity against human IGROV-1 cells
|
[PMID: 38316368] |
| K562 | GI50 |
0.01 μM
Compound: 12a
|
Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
|
[PMID: 38316368] |
| KM12 | GI50 |
0.74 μM
Compound: 12a
|
Antiproliferative activity against human KM12 cells
Antiproliferative activity against human KM12 cells
|
[PMID: 38316368] |
| LOX IMVI | GI50 |
0.2 μM
Compound: 12a
|
Antiproliferative activity against human LOX IMVI cells
Antiproliferative activity against human LOX IMVI cells
|
[PMID: 38316368] |
| M14 | GI50 |
0.16 μM
Compound: 12a
|
Antiproliferative activity against human M14 cells
Antiproliferative activity against human M14 cells
|
[PMID: 38316368] |
| Malme-3M | GI50 |
0.2 μM
Compound: 12a
|
Antiproliferative activity against human Malme-3M cells
Antiproliferative activity against human Malme-3M cells
|
[PMID: 38316368] |
| MCF7 | GI50 |
8.33 μM
Compound: 12a
|
Antiproliferative activity against human MCF7 cells
Antiproliferative activity against human MCF7 cells
|
[PMID: 38316368] |
| MDA-MB-231 | GI50 |
0.13 μM
Compound: 12a
|
Antiproliferative activity against human MDA-MB-231 cells
Antiproliferative activity against human MDA-MB-231 cells
|
[PMID: 38316368] |
| MDA-MB-435 | GI50 |
0.25 μM
Compound: 12a
|
Antiproliferative activity against human MDA-MB-435 cells
Antiproliferative activity against human MDA-MB-435 cells
|
[PMID: 38316368] |
| MDA-MB-468 | GI50 |
0.38 μM
Compound: 12a
|
Antiproliferative activity against human MDA-MB-468 cells
Antiproliferative activity against human MDA-MB-468 cells
|
[PMID: 38316368] |
| MOLT-4 | GI50 |
0.43 μM
Compound: 12a
|
Antiproliferative activity against human MOLT-4 cells
Antiproliferative activity against human MOLT-4 cells
|
[PMID: 38316368] |
| NCI/ADR-RES | GI50 |
3.53 μM
Compound: 12a
|
Antiproliferative activity against human NCI/ADR-RES cells
Antiproliferative activity against human NCI/ADR-RES cells
|
[PMID: 38316368] |
| NCI-H226 | GI50 |
0.41 μM
Compound: 12a
|
Antiproliferative activity against human NCI-H226 cells
Antiproliferative activity against human NCI-H226 cells
|
[PMID: 38316368] |
| NCI-H23 | GI50 |
0.499 μM
Compound: 12a
|
Antiproliferative activity against human NCI-H23 cells
Antiproliferative activity against human NCI-H23 cells
|
[PMID: 38316368] |
| NCI-H460 | GI50 |
0.43 μM
Compound: 12a
|
Antiproliferative activity against human NCI-H460 cells
Antiproliferative activity against human NCI-H460 cells
|
[PMID: 38316368] |
| NCI-H522 | GI50 |
0.3 μM
Compound: 12a
|
Antiproliferative activity against human NCI-H522 cells
Antiproliferative activity against human NCI-H522 cells
|
[PMID: 38316368] |
| OVCAR-3 | GI50 |
1.09 μM
Compound: 12a
|
Antiproliferative activity against human OVCAR-3 cells
Antiproliferative activity against human OVCAR-3 cells
|
[PMID: 38316368] |
| OVCAR-5 | GI50 |
0.54 μM
Compound: 12a
|
Antiproliferative activity against human OVCAR-5 cells
Antiproliferative activity against human OVCAR-5 cells
|
[PMID: 38316368] |
| OVCAR-8 | GI50 |
0.41 μM
Compound: 12a
|
Antiproliferative activity against human OVCAR-8 cells
Antiproliferative activity against human OVCAR-8 cells
|
[PMID: 38316368] |
| PC-3 | GI50 |
0.79 μM
Compound: 12a
|
Antiproliferative activity against human PC-3 cells
Antiproliferative activity against human PC-3 cells
|
[PMID: 38316368] |
| RXF 393 | GI50 |
0.094 μM
Compound: 12a
|
Antiproliferative activity against human RXF 393 cells
Antiproliferative activity against human RXF 393 cells
|
[PMID: 38316368] |
| SF-268 | GI50 |
0.49 μM
Compound: 12a
|
Antiproliferative activity against human SF-268 cells
Antiproliferative activity against human SF-268 cells
|
[PMID: 38316368] |
| SK-MEL-2 | GI50 |
0.092 μM
Compound: 12a
|
Antiproliferative activity against human SK-MEL-2 cells
Antiproliferative activity against human SK-MEL-2 cells
|
[PMID: 38316368] |
| SK-MEL-28 | GI50 |
0.24 μM
Compound: 12a
|
Antiproliferative activity against human SK-MEL-28 cells
Antiproliferative activity against human SK-MEL-28 cells
|
[PMID: 38316368] |
| SK-OV-3 | GI50 |
0.19 μM
Compound: 12a
|
Antiproliferative activity against human SK-OV-3 cells
Antiproliferative activity against human SK-OV-3 cells
|
[PMID: 38316368] |
| SN12C | GI50 |
0.17 μM
Compound: 12a
|
Antiproliferative activity against human SN12C cells
Antiproliferative activity against human SN12C cells
|
[PMID: 38316368] |
| SNB-19 | GI50 |
3.92 μM
Compound: 12a
|
Antiproliferative activity against human SNB-19 cells
Antiproliferative activity against human SNB-19 cells
|
[PMID: 38316368] |
| SNB-75 | GI50 |
0.29 μM
Compound: 12a
|
Antiproliferative activity against human SNB-75 cells
Antiproliferative activity against human SNB-75 cells
|
[PMID: 38316368] |
| SR | GI50 |
0.18 μM
Compound: 12a
|
Antiproliferative activity against human SR cells
Antiproliferative activity against human SR cells
|
[PMID: 38316368] |
| SW-620 | GI50 |
0.52 μM
Compound: 12a
|
Antiproliferative activity against human SW620 cells
Antiproliferative activity against human SW620 cells
|
[PMID: 38316368] |
| T47D | GI50 |
0.7 μM
Compound: 12a
|
Antiproliferative activity against human T47D cells
Antiproliferative activity against human T47D cells
|
[PMID: 38316368] |
| TK-10 | GI50 |
0.39 μM
Compound: 12a
|
Antiproliferative activity against human TK-10 cells
Antiproliferative activity against human TK-10 cells
|
[PMID: 38316368] |
| U-251 | GI50 |
0.55 μM
Compound: 12a
|
Antiproliferative activity against human U-251 cells
Antiproliferative activity against human U-251 cells
|
[PMID: 38316368] |
| UACC-257 | GI50 |
0.67 μM
Compound: 12a
|
Antiproliferative activity against human UACC-257 cells
Antiproliferative activity against human UACC-257 cells
|
[PMID: 38316368] |
| UO-31 | GI50 |
0.27 μM
Compound: 12a
|
Antiproliferative activity against human UO-31 cells
Antiproliferative activity against human UO-31 cells
|
[PMID: 38316368] |
In Vitro
Lck-IN-2 inhibits Lck phosphorylation and induces apoptosis in human colon cancer cells Colo201 in dose-dependent manner[1].
Lck-IN-2 reveals anti-proliferative potencies against various cancer cells, with GI50 of 0.01-8 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Colo201
-
Concentration:0-10 μM
-
Incubation Time:
-
Result:Reduced the Lck phosphorylation and increased levels of cleaved PARP in dose-dependent manner
Chemical Information
-
CAS No. 2615173-24-3
-
Masse moléculaire 596.64
-
Formule C31H32N8O5
-
SMILES
CC1=CC=C(C=C1N2CC3=C(N(C2=O)C)N=C(N=C3)NC4=CN=C(C=C4)C)NC(C5=CC=C(C(OCC(C)C)=C5)[N+]([O-])=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)