Reagents and instruments for immunology, cell biology and molecular biology.

Alectinib [1256580-46-7]

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Cat# HY-13011-5mg

Size : 5mg

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Description

Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC₅₀ of 1.9 nM and a K_d value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC₅₀s of 1 nM and 3.5 nM, respectively^[1]. Alectinib demonstrates effective central nervous system (CNS) penetration^[2].

IC₅₀ & Target

IC50: 1.9 nM(ALK), 1 nM (ALK^F1174L), 3.5 nM (ALK^R1275Q)^[1]
Kd: 2.4 nM (ALK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	> 1000 nM Compound: 1	Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	169 nM Compound: 1	Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 1	Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 1	Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 1	Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	207 nM Compound: 1	Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	3 nM Compound: 1	Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	72 nM Compound: 1	Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	9 nM Compound: 1	Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	90 nM Compound: 1	Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
KARPAS-299	IC₅₀	15 nM Compound: 3; CH5424802	Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
KARPAS-299	IC₅₀	3 nM Compound: Alectinib	Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
KARPAS-299	IC₅₀	3 nM Compound: 18a, CH5424802	Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay	[PMID: 22225917]
KARPAS-299	IC₅₀	47 nM Compound: 3	Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34176264]
Kelly	EC₅₀	434 nM Compound: 1	Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
NB1	IC₅₀	4.5 nM Compound: Alectinib	Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
NCI-H2228	IC₅₀	53 nM Compound: Alectinib	Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay	[PMID: 34402300]
NCI-H2228	IC₅₀	6.5 nM Compound: CH5424802	Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay	[PMID: 31425908]
NCI-H3122	IC₅₀	17.4 nM Compound: 3; CH5424802	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
NCI-H3122	IC₅₀	19 nM Compound: 5	Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs	[PMID: 26476749]
NCI-H3122	IC₅₀	45 nM Compound: 3	Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34176264]
NCI-H3122	EC₅₀	9 nM Compound: 1	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
NIH3T3	IC₅₀	132 nM Compound: 3; CH5424802	Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
NIH3T3	IC₅₀	32.3 nM Compound: 3; CH5424802	Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
SH-SY5Y	EC₅₀	1150 nM Compound: 1	Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-AS	EC₅₀	2139 nM Compound: 1	Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-FI	EC₅₀	2401 nM Compound: 1	Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-SH	EC₅₀	872 nM Compound: 1	Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SU-DHL-1	IC₅₀	20.5 nM Compound: 3; CH5424802	Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]

In Vitro

Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT^[1].
Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	0 nM,10 nM,100 nM, 1000 nM
Incubation Time:	2 hours
Result:	Inhibition of ALK phosphorylation and signal transduction.

Cell Viability Assay^[1]

Cell Line:	HCC827, A549, or NCIH522 cells
Concentration:	0-1000 nM
Incubation Time:	5 days
Result:	Reduced cell activity in a dose-dependent manner.

In Vivo

Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC₅₀ of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed^[1].

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

Animal Model:	SCID or nude mice bearing NCI-H2228 cells^[1]
Dosage:	0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg
Administration:	Oral administration; once daily; for 11 days
Result:	Resulted in dose-dependent tumor growth inhibition (EC₅₀ of 0.46 mg/kg) and tumor regression.

Clinical Trial

Molecular Weight

482.62

Formula

C₃₀H₃₄N₄O₂

CAS No.

1256580-46-7

Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC2=C(C3=C(N2)C(C)(C4=CC(N5CCC(CC5)N6CCOCC6)=C(C=C4C3=O)CC)C)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 4.33 mg/mL (8.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0720 mL	10.3601 mL	20.7202 mL
5 mM	0.4144 mL	2.0720 mL	4.1440 mL
10 mM	---	---	---

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.38 mg/mL (0.79 mM); Clear solution

This protocol yields a clear solution of ≥ 0.38 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.38 mg/mL (0.79 mM); Clear solution

This protocol yields a clear solution of ≥ 0.38 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 12.5 mg/mL (25.90 mM); Suspended solution; Need ultrasonic

Purity & Documentation

Purity: 99.78%

Data Sheet (277 KB) SDS (393 KB)

COA (248 KB) HNMR (141 KB) RP-HPLC (247 KB) MS (74 KB)

Handling Instructions (2659 KB)

References

[1]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690. [Content Brief]

[2]. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222. [Content Brief]

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