ALK-IN-22

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ALK-IN-22 (compound I-24) is a potent ALK inhibitor with IC₅₀ values of 2.3, 3.7 and 2.9 nM for ALK, ALK^L1196M and ALK^G1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research.

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

ALK-IN-22 Chemical Structure

CAS No. : 2468219-09-0

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Biological Activity
Purity & Documentation
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.39 μM Compound: I-24	Antiproliferative activity against EGFR positive human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against EGFR positive human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
BaF3	IC₅₀	> 1 μM Compound: I-24	Antiproliferative activity IL3 dependent human Ba/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity IL3 dependent human Ba/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
HCT-116	IC₅₀	1.34 μM Compound: I-24	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
HEK-293T	IC₅₀	> 10 μM Compound: I-24	Antiproliferative activity against human HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
Hep 3B2	IC₅₀	0.059 μM Compound: I-24	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
HT-29	IC₅₀	2.01 μM Compound: I-24	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
KARPAS-299	IC₅₀	0.011 μM Compound: I-24	Antiproliferative activity against NPM-ALK positive human KARPAS-299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against NPM-ALK positive human KARPAS-299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
MCF7	IC₅₀	2.16 μM Compound: I-24	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
MDA-MB-231	IC₅₀	1.88 μM Compound: I-24	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
NCI-H1581	IC₅₀	0.957 μM Compound: I-24	Antiproliferative activity against human NC-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NC-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
NCI-H2228	IC₅₀	0.037 μM Compound: I-24	Antiproliferative activity against EML4-ALK positive human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against EML4-ALK positive human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
NCI-H3122	IC₅₀	0.027 μM Compound: I-24	Antiproliferative activity against EML4-ALK positive human NC-H3122 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against EML4-ALK positive human NC-H3122 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]
PC-3	IC₅₀	1.38 μM Compound: I-24	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35691173]

In Vitro

ALK-IN-22 (compound I-24) (72 hours) has anti-proliferative activities against ALK-positive karpas299, H2228 and H3122 cell lines with IC₅₀ values of 11, 37 and 27 nM, respectively^[1].
ALK-IN-22 (compound I-24) (0-100 nM; 24 hours; H2228 cells) has inhibitory effect on ALK and downstream signaling AKT and ERK^[1].
ALK-IN-22 (compound I-24) (0-100 nM; 48 hours; H2228 cells) can induce apoptosis and achieve cell cycle arrest in G1 phase^[1].

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

Western Blot Analysis^[1]

Cell Line:	H2228 cells
Concentration:	0, 25, 50 and 100 nM
Incubation Time:	24 hours
Result:	Downregulated the phosphorylation level of ALK and blocked the expressions of ALK downstream key signaling AKT, ERK along with their activated forms in a dose-dependent fashion.

Apoptosis Analysis^[1]

Cell Line:	H2228 cells
Concentration:	0, 25, 50 and 100 nM
Incubation Time:	48 hours
Result:	The apoptotic rates were 14.23%, 23.94% and 31.70% at concentrations of 25 nM, 50 nM and 100 nM, respectively.

Cell Cycle Analysis^[1]

Cell Line:	H2228 cells
Concentration:	0, 25, 50 and 100 nM
Incubation Time:	48 hours
Result:	The percentage of cells in the G1 phase increased from 49.72% to 58.51% in a dose-dependent fashion.

In Vivo

ALK-IN-22 (compound I-24) (25-50 mg/kg; i.g.; Twice daily, for 14 days) has antitumor efficacy in vivo^[1].
ALK-IN-22 (compound I-24) (10 mg/kg; p.o.) shows the C_max and t_1/2 values of 345.7 ng/mL and 4.1 hours, respectively^[1].
ALK-IN-22 (compound I-24) (2 mg/kg; i.v.) shows the CL and t_1/2 values of 36.2 mL/min/kg and 2.5 hours, respectively^[1].

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

Animal Model:	Female BALB / c nude mice^[1]
Dosage:	25 and 50 mg/kg
Administration:	Intragastric; Twice daily, for 14 days.
Result:	The tumor growth inhibition (TGI) value of 50 mg/kg reached 93.5%.

Animal Model:

SD rats^[1]

Dosage:

2 and 10 mg/kg (Pharmacokinetic Analysis)

Administration:

Oral administration and intravenous injection

Result:

1.19

Parameter	F16	VP-16
Dose (i.v.) mg/kg	10	10
C_max (ng/mL)	26952	17712
T_max (min)	5	5
AUC_plasma (min*ng/mL)	2878363	409528
T_1/2 (min)	151	45
Vd (L/Kg)	0.2341	0.432
CL (L/min/kg)	0.001	0.007

Molecular Weight

477.95

Formula

C₂₄H₂₄ClN₇O₂

CAS No.

2468219-09-0

SMILES

O=C(C1=C(C)NC2=C1C=CC(NC3=NC=C(Cl)C(NC4=CC=CC=C4C(NC)=O)=N3)=C2)N(C)C

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]. Thacker PS, et al. Synthesis and biological evaluation of some coumarin hybrids as selective carbonic anhydrase IX and XII inhibitors. Bioorg Chem. 2020 Nov;104:104272. [Content Brief]

ALK-IN-22 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:

ALK-IN-222468219-09-0Anaplastic lymphoma kinase (ALK)ApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246apoptosisALKphosphorylationantitumorInhibitorinhibitorinhibit

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