Art. -Nr.: HY-13011

Alectinib

(Synonyms: CH5424802; RO5424802; RG7853)

44 Cited Publications

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Based on 44 publication(s) in Google Scholar

Alectinib (CH5424802; RO5424802; RG7853) 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. Alectinib demonstrates effective central nervous system (CNS) penetration.

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Reinheit: 99.78%
CAS. Nr.: 1256580-46-7
Formel: C₃₀H₃₄N₄O₂
Molecular Weight:482.62

Speicherung:

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

Alectinib Chemical Structure

CAS. Nr.: 1256580-46-7

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (44)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
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Biologische Aktivität

Beschreibung

Alectinib (CH5424802; RO5424802; RG7853) 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	>2000 nM Compound: CH5424802; AF-802	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	>2000 nM Compound: CH5424802; AF-802	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	>2000 nM Compound: CH5424802; AF-802	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
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 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	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	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]
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	2067 nM Compound: Alectinib	Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth in presence of IL-3 Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth in presence of IL-3	[PMID: 27780853]
HCC78	IC₅₀	>1000 nM Compound: CH5424802; AF-802	Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
HCC78	IC₅₀	>10000 nM Compound: CH5424802; AF-802	Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
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	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: 4; CH5424802	Antiproliferative activity against human KARPAS299 cells Antiproliferative activity against human KARPAS299 cells	[PMID: 31419130]
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]
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]
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	4.5 nM Compound: 4; CH5424802	Inhibition of EML4/ALK in human NCI-H2228 cells Inhibition of EML4/ALK in human NCI-H2228 cells	[PMID: 31419130]
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-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-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	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]
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	9 nM Compound: 4; CH5424802	Cytotoxicity against human NCI-H3122 cells Cytotoxicity against human NCI-H3122 cells	[PMID: 31419130]
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]
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]
SR	IC₅₀	3.4 nM Compound: Alectinib	Antiproliferative activity against ALK positive human SR cells Antiproliferative activity against ALK positive human SR cells	[PMID: 33751979]
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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1256580-46-7
Appearance Solid
Molecular Weight 482.62
Formel C₃₀H₃₄N₄O₂
Color White to light yellow
SMILES

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

CH5424802; RO5424802; RG7853
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (44)

All WB

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Science

Tracking cancer drugs in living cells by thermal profiling of the proteome. [Abstract]

2014 Oct 3;346(6205):1255784. PMID: 25278616
Cell

GUK1 activation is a metabolic liability in lung cancer. [Abstract]

2025 Mar 6;188(5):1248-1264.e23. PMID: 39919745
Cancer Discov

EML4-ALK mediates resistance to KRAS G12C inhibition and induces an oncogenic dependency by rewiring signaling through the wild-type RAS pathway. [Abstract]

2026 Jun 22. PMID: 42329099
Cancer Discov

NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations. [Abstract]

2024 Sep 13:OF1-OF20. PMID: 39269178
Cancer Discov

Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound ALK Mutations in ALK-Positive Lung Cancer. [Abstract]

2018 Jun;8(6):714-729. PMID: 29650534
Cancer Discov

Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer. [Abstract]

2016 Oct;6(10):1118-1133. PMID: 27432227
Nat Cancer

Analysis of lorlatinib analogs reveals a roadmap for targeting diverse compound resistance mutations in ALK-positive lung cancer. [Abstract]

2022 Jun;3(6):710-722. PMID: 35726063
Cancer Res

Mesenchymal-Type Neuroblastoma Cells Escape ALK Inhibitors. [Abstract]

2022 Feb 1;82(3):484-496. PMID: 34853072
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Multiscale profiling of protease activity in cancer. [Abstract]

2022 Oct 3;13(1):5745. PMID: 36192379
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Leukemia

Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]

2025 Aug 14. PMID: 40813622
Cell Discov

Phase separation of EML4-ALK in firing downstream signaling and promoting lung tumorigenesis. [Abstract]

2021 May 11;7(1):33. PMID: 33976114
Cell Rep Med

STAT3 couples activated tyrosine kinase signaling to the oncogenic core transcriptional regulatory circuitry of anaplastic large cell lymphoma. [Abstract]

2024 Mar 19;5(3):101472. PMID: 38508140
Cell Rep Med

Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]

2023 Feb 21;4(2):100911. PMID: 36657446
Cancer Lett

The second-generation ALK inhibitor alectinib effectively induces apoptosis in human neuroblastoma cells and inhibits tumor growth in a TH-MYCN transgenic neuroblastoma mouse model. [Abstract]

2017 Aug 1:400:61-68. PMID: 28455243

Alectinib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Aug 1:400:61-68. [Abstract]

Alectinib inhibits PI3K/Akt/mTOR signaling and induces apoptosis in NB cells. NB-19, Kelly, IMR-32, SH-SY5Y, SK-N-AS and LA-N-6 cells are treated with 10 mM alectinib for various time points as indicated. The anti-b-Actin antibody is used as a loading control for whole cell extracts.

Alectinib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Aug 1:400:61-68. [Abstract]

In contrast to tumors treated with DMSO, tumors treated with Alectinib exhibits significantly decreased levels of p-Akt and p-S6. Furthermore, increased PARP and Caspase 3 cleavages are observed in tumors treated with Alectinib compared to controls.
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Neoplasia

ALK inhibitors downregulate the expression of death receptor 4 in ALK-mutant lung cancer cells via facilitating Fra-1 and c-Jun degradation and subsequent AP-1 suppression. [Abstract]

2023 Aug:42:100908. PMID: 37192591
Oncogene

ALK fusion promotes metabolic reprogramming of cancer cells by transcriptionally upregulating PFKFB3. [Abstract]

2022 Sep;41(40):4547-4559. PMID: 36064579
Aging Cell

The neuronal receptor tyrosine kinase Alk is a target for longevity. [Abstract]

2020 May;19(5):e13137. PMID: 32291952
Cell Death Discov

The p53 activator overcomes resistance to ALK inhibitors by regulating p53-target selectivity in ALK-driven neuroblastomas. [Abstract]

2018 May 10:4:56. PMID: 29760954

Alectinib purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2018 May 10:4:56. [Abstract]

NB39-nu cells are treated with either 1000 nM Crizotinib (CR) or Alectinib (AL) for the indicated times and subjected to immunoblot analysis. CLTC is the loading control.
Sci Signal

Host protein kinases required for SARS-CoV-2 nucleocapsid phosphorylation and viral replication. [Abstract]

2022 Oct 25;15(757):eabm0808. PMID: 36282911
Pharmaceutics

Evaluation of Alectinib Metabolic Stability in HLMs Using Fast LC-MS/MS Method: In Silico ADME Profile, P450 Metabolic Lability, and Toxic Alerts Screening. [Abstract]

2023 Oct 11;15(10):2449. PMID: 37896209
Microchem J

2025 Nov 3;219:116046.
Biomolecules

Lysophosphatidic Acid Stimulates Mitogenic Activity and Signaling in Human Neuroblastoma Cells through a Crosstalk with Anaplastic Lymphoma Kinase. [Abstract]

2024 May 28;14(6):631. PMID: 38927035
BMC Chem

Integrating analytical quality by design into bioanalytical method development: an HPLC-FLD method for quantification of alectinib in biological matrix. [Abstract]

2025 Aug 22;19(1):248. PMID: 40847406
Cancer Sci

APE1 Attenuates ALK Tyrosine Kinase Inhibitors Sensitivity in NPM1-ALK Positive Anaplastic Large Cell Lymphoma. [Abstract]

2025 Jul 23. PMID: 40702700
Transl Oncol

Anti-epidermal growth factor vaccine antibodies increase the antitumor activity of kinase inhibitors in ALK and RET rearranged lung cancer cells. [Abstract]

2021 Jan;14(1):100887. PMID: 33129112
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Heliyon

Quality by design-based approach for the development of an analytical method for quantifying ponatinib in rat plasma. [Abstract]

2024 Sep 28;10(19):e38637. PMID: 39403541
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
PLoS One

Inhibition of the anti-apoptotic protein BCL2 in EML4-ALK cell models as a second proposed therapeutic target for non-small cell lung cancer. [Abstract]

2025 Jan 21;20(1):e0308747. PMID: 39836700
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
Cell Physiol Biochem

Inhibition of Erythrocyte Cell Membrane Scrambling Following Energy Depletion and Hyperosmotic Shock by Alectinib. [Abstract]

2018;51(5):1996-2009. PMID: 30522123
Biol Pharm Bull

Evaluation of Drug-Induced Kidney Injury by Primary Culture of Rat Kidney Tissue Slices Using Oxygen-Permeable Polyolefin Plate with Low Drug Adsorption. [Abstract]

2026;49(1):122-129. PMID: 41565252
Biomed Chromatogr

Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method to quantify the small molecule inhibitors adagrasib, alectinib, brigatinib, capmatinib, crizotinib, lorlatinib, selpercatinib, and sotorasib in human plasma. [Abstract]

2024 Oct;38(10):e5986. PMID: 39136165
bioRxiv

2025 Dec 5.
Patent

US20250003968A1.
Research Square Preprint

2024 Nov 26.
bioRxiv

The FDA-approved drug Alectinib compromises SARS-CoV-2 nucleocapsid phosphorylation and inhibits viral infection in vitro. [Abstract]

2020 Dec 16:2020.08.14.251207. PMID: 32817937
University of California

2024.
bioRxiv

November 12, 2021.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0720 mL

10.3601 mL

20.7202 mL

5 mM

0.4144 mL

2.0720 mL

4.1440 mL

10 mM

---

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Working Solution

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
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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)

Verweise

[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]

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.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0720 mL	10.3601 mL	20.7202 mL	51.8006 mL
DMSO	5 mM	0.4144 mL	2.0720 mL	4.1440 mL	10.3601 mL

Keywords

Alectinib

44 Cited Publications

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Alectinib

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Publications Citing Use of MedChemExpress (MCE) Alectinib

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Publications (44)

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Complete Stock Solution Preparation Table

Alectinib Related Classifications

HY-13011 Related Classifications