Name: Alectinib (CH5424802) hydrochloride
Brand: Selleck Chemicals
SKU: S5232
Availability: InStock
Rating: 5 (27 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	EGFR VEGFR FGFR PDGFR c-Met Src MEK CSF-1R FLT3 HER2
Other ALK Inhibitors	TAE684 (NVP-TAE684) GSK1838705A Repotrectinib (TPX-0005) Ensartinib dihydrochloride AZD3463 AP26113-analog (ALK-IN-1) ASP3026 NVL-655 (Neladalkib) HG-14-10-04 X-376

Solubility

In vitro
Batch:

DMSO : 2 mg/mL (3.85 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.1mg/ml (0.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 2 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.014mg/ml (0.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 0.28 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	519.08	Formula	C₃₀H₃₄N₄O₂.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1256589-74-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AF802, RO5424802, RG-7853			SMILES	CCC1=CC2=C(C=C1N3CCC(CC3)N4CCOCC4)C(C5=C(C2=O)C6=C(N5)C=C(C=C6)C#N)(C)C.Cl

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	ALK (Cell-free) 1.9 nM
In vitro	Alectinib inhibits ALK with an IC50 value of 1.9 nmol/L and shows higher selectivity for ALK than for a number of other serine/tyrosine kinases. It also inhibits the ALK gatekeeper mutation L1196M with an IC50 of 1.56 nmol/L. Alectinib is effective with PF-02341066-resistant ALK mutations L1196M, F1174L, R1275Q and C1156Y. In the KARPAS-299 (lymphoma), NB-1 (neuroblastoma) and NCI-H2228 (lung cancer) ALK-positive cell lines, alectinib inhibits cell proliferation with IC50 values of 3, 4.5 and 53 nmol/L, respectively.
In vivo	Alectinib dose-dependently inhibits EML4-ALK positive NCI-H2228 xenograft model at doses ranging from 2 to 20 mg/kg p.o., q.d. Significant efficacy is also achieved in the EML4-ALK L1196M-driven tumors. It has antitumor activity against cancers with ALK gene alterations.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26579422/ [2] https://pubmed.ncbi.nlm.nih.gov/24887559/ [3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5382559/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2023-02-21)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05725200	RECRUITING	Metastatic Colorectal Cancer	Oslo University Hospital	2022-09-27	PHASE2
NCT04589845	ACTIVE_NOT_RECRUITING	Solid Tumors	Hoffmann-La Roche	2021-01-18	PHASE2
NCT04774718	ACTIVE_NOT_RECRUITING	ALK Fusion-positive Solid or CNS Tumors	Hoffmann-La Roche	2021-09-14	PHASE1; PHASE2
NCT07001384	RECRUITING	Anaplastic Lymphoma Kinase; Anaplastic Large Cell Lymphoma	Memorial Sloan Kettering Cancer Center	2025-08-08	PHASE1
NCT05170204	ACTIVE_NOT_RECRUITING	Non-Small Cell Lung Cancer	Hoffmann-La Roche	2022-11-01	PHASE3
NCT07573696	NOT_YET_RECRUITING	Nonsmall Cell Lung Cancer Stage III	Wen-zhao ZHONG	2026-06-15	PHASE2

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Handling Instructions

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Alectinib (CH5424802) hydrochloride ALK inhibitor

Chemical Structure

Molecular Weight: 519.08