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Cat. No.: HY-151155

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ALK-IN-23

ALK-IN-23 is a potent ALK inhibitor with IC₅₀ values of 1.6 nM, 0.71 nM and 1.3 nM for ALK^WT, ALK^L1196M and ALK^G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity.

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CAS No.: 3033549-18-4
화학식: C₂₆H₂₉ClN₈O₃S
분자량:569.08

보관:

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

Data Sheet (274 KB)

ALK-IN-23 Chemical Structure

CAS No.: 3033549-18-4

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

IC₅₀: 1.6 nM (ALK^WT), 0.71 nM (ALK^L1196M), 1.3 nM (ALK^G1202R)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1.33 μM Compound: Y28	Antiproliferative activity against EGFR-positive human A549 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against EGFR-positive human A549 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
HCT-116	IC₅₀	1.56 μM Compound: Y28	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
KARPAS-299	IC₅₀	0.015 μM Compound: Y28	Antiproliferative activity against NPM-ALK-positive human KARPAS-299 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against NPM-ALK-positive human KARPAS-299 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
MCF7	IC₅₀	2.22 μM Compound: Y28	Antiproliferative activity against human MCF7 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H1581	IC₅₀	1.87 μM Compound: Y28	Antiproliferative activity against human NCI-H1581 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human NCI-H1581 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H2228	IC₅₀	0.017 μM Compound: Y28	Antiproliferative activity against EML4-ALK-positive human NCI-H2228 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against EML4-ALK-positive human NCI-H2228 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H3122	IC₅₀	0.012 μM Compound: Y28	Antiproliferative activity against EML4-ALK-positive human NCI-H3122 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against EML4-ALK-positive human NCI-H3122 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
NCI-H460	IC₅₀	8.21 μM Compound: Y28	Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]
PC-3	IC₅₀	1.23 μM Compound: Y28	Antiproliferative activity against human PC-3 cells incubated for 72 hrs and measured by CCK-8 assay Antiproliferative activity against human PC-3 cells incubated for 72 hrs and measured by CCK-8 assay	[PMID: 35939995]

In Vitro

ALK-IN-23 (compound Y28) (0-5 μM; 72h) has highly inhibitory activity against H3122, H2228, Karpas299 and A549^[1].
ALK-IN-23 (25-100 nM; 3 days) clearly reduces the number of H2228 cell colonies, and almost completely abolishes the formation of colonies at 100 nM^[1].
ALK-IN-23 (100-200 nM; 48 h) facilitates the apoptosis of H2228 cells^[1].
ALK-IN-23 (5-10 nM; 24 and 48 h) is effective to block the migration of most cells at a dose of 10 nM^[1].
ALK-IN-23 (25-100 nM; overnight) significantly increases the percentage of cells in the G2 phase^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

H3122, H2228, Karpas299 and A549
Concentration:

0-5 μM
Incubation Time:

72 h
Result:

Exhibited highly inhibitory activity against H3122, H2228, Karpas299 and A549 with IC₅₀s of 12 nM, 17 nM, 15 nM and 1.33 μM.

Apoptosis Analysis^[1]

Cell Line:

H2228 cells
Concentration:

100 nM, 200 nM
Incubation Time:

48 h
Result:

Facilitated the apoptosis of H2228 cells in a dose dependent manner and exhibited a more pro-apoptotic effect than that of Ceritinib (HY-15656).

Cell Migration Assay ^[1]

Cell Line:

H2228 cells
Concentration:

5 nM and 10 nM
Incubation Time:

24 and 48 h
Result:

Blocked the migration of most cells at a dose of 10 nM (migration rate: 24 h 2.31%, 48 h: 5.01%).

Cell Cycle Analysis^[1]

Cell Line:

H2228 cells
Concentration:

25 nM, 50 nM, 100 nM
Incubation Time:

Overnight
Result:

Significantly increased the percentage of cells in the G2 phase from 11.28% to 73.23% in a dramatic dose-dependent manner, accompanied by a resultant loss of G1-and S-phase populations.

In Vivo

ALK-IN-23 notes a moderate half-life of 16.3 min and a high intrinsic liver clearance of 152.9 mL/min/kg in rats^[1].
ALK-IN-23 (25 and 50 mg/kg; IG; once every 2 days; for 14 days) exhibited gentle antitumor efficacy and no significant weight loss in H2228 xenograft mice model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female BALB/c nude mice (5×10⁶ cells H2228 cells suspended in serum-free media were injected into the flanks)^[1]
Dosage:

25 and 50 mg/kg
Administration:

IG; once every 2 days; for 14 days
Result:

Presented moderate antitumor efficacy with the tumor growth inhibition (TGI) of 70.46% at 50 mg/kg.
Possessed gentle antitumor efficacy and exhibited no significant weight loss.

Chemical Information

CAS No. 3033549-18-4
분자량 569.08
화학식 C₂₆H₂₉ClN₈O₃S
SMILES

CC(S(=O)(C1=CC=CC=C1NC2=NC(NC3=CC=C4C(NN=C4NC(CN5CCCC5)=O)=C3)=NC=C2Cl)=O)C
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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]. Yang J, et al. Design, synthesis and antitumor evaluation of ATP dual-mimic 2,4-diarylaminopyrimidine and aminoindazole conjugates as potent anaplastic lymphoma kinase inhibitors. Eur J Med Chem. 2022 Jul 31;241:114626. [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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MOQ

Minimum order quantity

100 mg

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