Cat. No.: HY-163278

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.

For research use only. We do not sell to patients.

CAS No.: 2615173-24-3
Formula: C₃₁H₃₂N₈O₅
Molecular Weight:596.64

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (266 KB)

Lck-IN-2 Chemical Structure

CAS No.: 2615173-24-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Lck

10.6 nM (IC₅₀)

All Src Isoforms :

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.

Western Blot Analysis^[1]

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
Molecular Weight 596.64
Formula 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Hyun Ji S, et al., Identification of 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one scaffolds as potent Lck inhibitors as anti-cancer agents. Bioorg Med Chem Lett. 2024 Feb 3:129645. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Lck-IN-2

All Src Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Lck-IN-2 Related Classifications

HY-163278 Related Classifications