Lck-IN-2

Cat. No.: HY-163278: Data Sheet Handling Instructions
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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.

Lck-IN-2 Chemical Structure

CAS No. : 2615173-24-3

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•Related Small Molecules:

•Related Proteins:

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Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

Biological Activity
Purity & Documentation
References
Customer Review

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]
HT-29	GI₅₀	0.41 μM Compound: 12a	Antiproliferative activity against human HT-29 cells Antiproliferative activity against human HT-29 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]
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]
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]
Malme-3M	GI₅₀	0.2 μM Compound: 12a	Antiproliferative activity against human Malme-3M cells Antiproliferative activity against human Malme-3M 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]
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]
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

Molecular Weight

596.64

Formula

C₃₁H₃₂N₈O₅

CAS No.

2615173-24-3

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

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]

Lck-IN-2 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lck-IN-22615173-24-3SrcApoptosisLymphocyte-specific protein tyrosine kinaseLckColo201colon cancerInhibitorinhibitorinhibit

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