Alectinib
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 Kd 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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.78%
- CAS No.: 1256580-46-7
- 화학식: C30H34N4O2
- 분자량:482.62
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Alectinib
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Science. 2014 Oct 3;346(6205):1255784. [Abstract]
- Cell. 2025 Mar 6;188(5):1248-1264.e23. [Abstract]
- Cancer Discov. 2026 Jun 22. [Abstract]
- Cancer Discov. 2024 Sep 13:OF1-OF20. [Abstract]
- Cancer Discov. 2018 Jun;8(6):714-729. [Abstract]
- Cancer Discov. 2016 Oct;6(10):1118-1133. [Abstract]
- Nat Cancer. 2022 Jun;3(6):710-722. [Abstract]
- Cancer Res. 2022 Feb 1;82(3):484-496. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2022 Oct 3;13(1):5745. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Leukemia. 2025 Aug 14. [Abstract]
- Cell Discov. 2021 May 11;7(1):33. [Abstract]
- Cell Rep Med. 2024 Mar 19;5(3):101472. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Cancer Lett. 2017 Aug 1:400:61-68. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Neoplasia. 2023 Aug:42:100908. [Abstract]
- Oncogene. 2022 Sep;41(40):4547-4559. [Abstract]
- Aging Cell. 2020 May;19(5):e13137. [Abstract]
- Cell Death Discov. 2018 May 10:4:56. [Abstract]
- Sci Signal. 2022 Oct 25;15(757):eabm0808. [Abstract]
- Pharmaceutics. 2023 Oct 11;15(10):2449. [Abstract]
- Microchem J. 2025 Nov 3;219:116046.
- Biomolecules. 2024 May 28;14(6):631. [Abstract]
- BMC Chem. 2025 Aug 22;19(1):248. [Abstract]
- Cancer Sci. 2025 Jul 23. [Abstract]
- Transl Oncol. 2021 Jan;14(1):100887. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Heliyon. 2024 Sep 28;10(19):e38637. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- PLoS One. 2025 Jan 21;20(1):e0308747. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Cell Physiol Biochem. 2018;51(5):1996-2009. [Abstract]
- Biol Pharm Bull. 2026;49(1):122-129. [Abstract]
- Biomed Chromatogr. 2024 Oct;38(10):e5986. [Abstract]
- bioRxiv. 2025 Dec 5.
- Patent. US20250003968A1.
- Research Square Preprint. 2024 Nov 26.
- bioRxiv. 2020 Dec 16:2020.08.14.251207. [Abstract]
- University of California. 2024.
- bioRxiv. November 12, 2021.
-
WB
-
WB
-
WB
Biological Activity
IC50: 1.9 nM(ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)[1]
Kd: 2.4 nM (ALK)[1]
|
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] |
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.
-
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 Line:HCC827, A549, or NCIH522 cells
-
Concentration:0-1000 nM
-
Incubation Time:5 days
-
Result:Reduced cell activity in a dose-dependent manner.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1256580-46-7
-
Appearance Solid
-
분자량 482.62
-
화학식 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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (44)
-
Journal Impact Factor
-
Most Recent
-
Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Science
2014 Oct 3;346(6205):1255784. PMID: 25278616 -
Cell
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
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
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
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 -
-
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
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
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 -
-
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 12.5 mg/mL (25.90 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
-
Data Sheet (277 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]
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.
| 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 |
| 5 mM | 0.4144 mL | 2.0720 mL | 4.1440 mL | 10.3601 mL |