ホームページ Protein Tyrosine Kinase ALK inhibitor Alectinib For research use only.

Alectinib

別名：AF-802, RG-7853,CH5424802

Alectinib is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429.

Alectinib化学構造

CAS No. 1256580-46-7

サイズ 価格(税別) 在庫状況
JPY 25500 国内在庫あり
JPY 115500 国内在庫あり
JPY 295500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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製品安全説明書

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Alectinib関連製品

シグナル伝達経路

ALK Signaling Pathways

ALKシグナル伝達経路

ALK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
NIH/3T3 Antitumor assay 50 mg/kg 10 days Antitumor activity against mouse NIH/3T3 cells expressing EML4-ALK L1196M mutant xenografted in nude mouse assessed as tumor stasis at 50 mg/kg, po qd administered for 10 days 27131066
NIH/3T3 Antitumor assay 50 mg/kg 10 days Antitumor activity against mouse NIH/3T3 cells expressing EML4-ALK L1196M mutant xenografted in nude mouse assessed as partial tumor regression at 50 mg/kg, po qd administered for 10 days 27131066
MKN-45 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
NCI-H1993 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
NCI-H2009 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
Calu-1 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
NCI-H23 Growth inhibitory assay ~10 μM IC50=3600 nM 21575866
PC-1 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
Calu-3 Growth inhibitory assay ~10 μM IC50=>10,000 nM 21575866
NCI-H2228 Growth inhibitory assay ~10 μM IC50=53 nM 21575866
SK-N-FI Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
KELLY Growth inhibitory assay ~10 μM IC50=62 nM 21575866
NB-1 Growth inhibitory assay ~10 μM IC50=4.5 nM 21575866
HDLM-2 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
SR Growth inhibitory assay ~10 μM IC50=6.9 nM 21575866
KARPAS-299 Growth inhibitory assay ~10 μM IC50=3 nM 21575866
NCI-H2228 Kinase assay ~1 μM prevents autophosphorylation of ALK 21575866
SNU-5 Growth inhibitory assay ~10 μM IC50=1800 nM 21575866
KATO-III Growth inhibitory assay ~10 μM IC50=7900 nM 21575866
SK-BR-3 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
BT-483 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
PC-3 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
22Rv1 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
U-87 MG Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
H3122 Growth inhibitory assay ~10 μM IC50=33 nM 25096400
LC-2/ad Apoptosis assay ~1 μM induces apoptosis 25349307
LC-2/ad Function assay ~1 μM inhibits the MAPK signaling pathway 25349307
Ba/F3 Function assay ~1 μM suppresses phosphorylation of ERK and increases the abundance of BIM 25349307
SNU-2535 Growth inhibitory assay ~10 μM IC50=33.1 nM 26849637
SNU-2535 Kinase assay ~1 μM inhibits the phosphorylation of ALK and its downstream molecules ERK1/2 and AKT 26849637
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.002 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.002 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.002 μM. 26568289
KARPAS299 Antiproliferative assay 96 hrs Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay, IC50 = 0.003 μM. 22225917
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.003 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.009 μM. 26568289
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.009 μM. 26568289
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.015 μM. 27131066
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.0174 μM. 27131066
SUP-M2 Antiproliferative assay 72 hrs Antiproliferative activity against human SUP-M2 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.0179 μM. 27131066
NCI-H3122 Function assay 72 hrs Inhibition of ALK expressed in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB/CCK-8 assay, IC50 = 0.019 μM. 27131066
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs, IC50 = 0.019 μM. 26476749
SU-DHL1 Antiproliferative assay 72 hrs Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.0205 μM. 27131066
NIH/3T3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay, IC50 = 0.0323 μM. 27131066
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.072 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.09 μM. 26568289
NIH/3T3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay, IC50 = 0.132 μM. 27131066
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.169 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.207 μM. 26568289
DFCI114 Antiproliferative assay 72 hrs Antiproliferative activity against human DFCI114 cells expressing EML4-ALK G1269A mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.207 μM. 26568289
CHLA20 Antiproliferative assay 72 hrs Antiproliferative activity against human CHLA20 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.43 μM. 26568289
Kelly Antiproliferative assay 72 hrs Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.434 μM. 26568289
DFCI76 Antiproliferative assay 72 hrs Antiproliferative activity against human DFCI76 cells expressing EML4-ALK L1152R mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.511 μM. 26568289
LAN5 Antiproliferative assay 72 hrs Antiproliferative activity against human LAN5 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.617 μM. 26568289
SMS-KCNR Antiproliferative assay 72 hrs Antiproliferative activity against human SMS-KCNR cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.765 μM. 26568289
SK-N-SH Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.872 μM. 26568289
SH-SY5Y Antiproliferative assay 72 hrs Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.15 μM. 26568289
SK-N-BE(2) Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-BE(2) cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.554 μM. 26568289
LAN1 Antiproliferative assay 72 hrs Antiproliferative activity against human LAN1 cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 2.004 μM. 26568289
SK-N-AS Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 2.139 μM. 26568289
SK-N-FI Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 2.401 μM. 26568289
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生物活性

製品説明 Alectinib is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429.
Targets
ALK (F1174L) [1]
(Cell-free assay)		 ALK [1]
(Cell-free assay)		 ALK (R1275Q) [1]
(Cell-free assay)
1 nM 1.9 nM 3.5 nM
In Vitro
In vitro The dissociation constant (KD) value of CH5424802 for ALK in an ATP-competitive manner is 2.4 nM. CH5424802 has substantial inhibitory potency against both native ALK and L1196M with Ki of 0.83 nM and 1.56 nM, respectively. CH5424802 prevents autophosphorylation of ALK in NCI-H2228 NSCLC cells expressing EML4-ALK. CH5424802 also suppresses the phosphorylation of STAT3 and AKT, but not of ERK1/2. CH5424802 completely inhibits the phosphorylation of STAT3 at Tyr705. CH5424802 is preferentially efficacious against NCI-H2228 cells expressing EML4-ALK, but not ALK fusion-negative NSCLC cell lines, including HCC827 cells (EGFR exon 19 deletion), A549 cells (KRAS mutant), or NCI-H522 cells (EGFR wild-type, KRAS wild-type, and ALK wild-type) in monolayer culture. CH5424802 elicits an apoptotic marker—caspase-3/7-like activation—in NCI-H2228 spheroid cells. CH5424802 blocks the growth of two lymphoma lines, KARPAS-299 and SR, with NPM-ALK fusion protein but does not influence the growth of an HDLM-2 lymphoma line without ALK fusion. [1] CH5424802 displays high target selectivity and the stronger anti-proliferative activity against KARPAS-299. CH5424802 inhibits KAPRAS-299 with an IC50 of 3 nM, and KDR with IC50 of 1.4 μM. The metabolic stability of CH5424802 is very high.[2]
Kinase Assay Kinase inhibitory assays in Vitro
The inhibitory ability against each kinase except for MEK1 and Raf-1 is evaluated by examining their ability to phosphorylate various substrate peptides in the presence of CH5424802 using time-resolved fluorescence resonance energy transfer (TR-FRET) assay or fluorescence polarization (FP) assay. The inhibitory activity against MEK1 is evaluated by quantitative analysis of the phosphorylation of a substrate peptide by a recombinant ERK2 protein in the presence of CH5424802. The inhibitory activity against Raf-1 is evaluated by examining the ability of the kinases to phosphorylate MEK1 in the presence of CH5424802.
細胞実験 細胞株 NSCLC, A549 and HCC827 cell lines
濃度 0-1 μM
反応時間 5 days
実験の流れ Cells including NSCLC, A549 and HCC827 are seeded in 96-well plates overnight and incubated with various concentrations of CH5424802 for the indicated time. For spheroid cell growth inhibition assay, cells are seeded on spheroid plates, incubated overnight, and then treated with compound for the indicated times. The viable cells are measured by the Luminescent Cell Viability Assay. Caspase-3/7 assay is evaluated using the Caspase-Glo 3/7 Assay Kit.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot pALK / ALK / pAKT / AKT / pERK / ERK / pS6 / S6 PARP / cleaved PARP / Akt / caspase 3 / Cleaved caspase 3 pROS1 / ROS1 / pSTAT3 / STAT3 p-EGFR Tyr1068 / EGFR / p-HER3 Tyr1222 / HER3 / p-IGF-1R Tyr1135 / IGF-1R 25228534
Growth inhibition assay Cell viability 25228534
In Vivo
In Vivo Oral administration of CH5424802 dose-dependently inhibits tumor growth with an ED50 of 0.46 mg/kg and tumor regression. Treatment of 20 mg/kg CH5424802 reveals rapid tumor regression by 168%, the tumor volume in any mouse is <30 mm3 after 11 days of treatment (at day 28), a potent antitumor effect is maintained, and tumor regrowth does not occur throughout the 4-week drug-free period. The half-life and the oral bioavailability of CH5424802 in mice are 8.6 hours and 70.8%, respectively. At a repeated dose of 6 mg/kg, the mean plasma levels reached 1.7, 1.5, and 0.3 nM at 2, 7, and 24 hours post-dose, respectively. Administration of CH5424802 leads to tumor growth prevention and tumor regression. Tumor growth inhibition at 20 mg/kg is 119% for KARPAS-299 and 104% for NB-1 on day 20. CH5424802 inhibits the phosphorylation of STAT3 in a dose-dependent manner (2–20 mg/kg). A partial decrease in AKT phosphorylation is also observed in CH5424802-treated xenograft tumors. [1]
動物実験 動物モデル SCID or nude mice bearing NCI-H2228
投与量 20 mg/kg
投与経路 Oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05987956 Not yet recruiting
Non-small Cell Lung Cancer
Han Xu M.D. Ph.D. FAPCR Sponsor-Investigator IRB Chair|Medicine Invention Design Inc
 March 8 2024 Phase 2|Phase 3
NCT05987644 Recruiting
Lung Cancer|NSCLC|Brain Metastases
Joshua Palmer|Genentech Inc.|Hoosier Cancer Research Network
 January 2024 Phase 1|Phase 2
NCT05770037 Recruiting
Solid Tumor|Haematological Malignancy|Malignant Neoplasm|Lymphoproliferative Disorders|Neoplasms by Histologic Type|Neoplasms by Site|Cancer|Anaplastic Large Cell Lymphoma|Lymphoma|Renal Cell Carcinoma|Neuroblastoma
Cancer Research UK|University of Manchester|University of Birmingham|Royal Marsden NHS Foundation Trust|Hoffmann-La Roche
 December 18 2023 Phase 2|Phase 3
NCT05710133 Not yet recruiting
NSCLC
The Netherlands Cancer Institute
 March 1 2023 Not Applicable
NCT05525338 Recruiting
Drug Monitoring|Carcinoma Non-Small-Cell Lung|Lung Cancer|Anaplastic Lymphoma Kinase Gene Mutation|Anaplastic Lymphoma Kinase Gene Translocation
University Medical Center Groningen|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Erasmus Medical Center|Maastricht University Medical Center|Radboud University Medical Center|The Netherlands Cancer Institute|Leiden University Medical Center
 March 23 2022 Phase 4
NCT04774718 Recruiting
ALK Fusion-positive Solid or CNS Tumors
Hoffmann-La Roche
 September 14 2021 Phase 1|Phase 2

化学情報

分子量 482.62 化学式

C30H34N4O2
CAS No. 1256580-46-7 SDF Download Alectinib SDFをダウンロードする
Smiles CCC1=CC2=C(C=C1N3CCC(CC3)N4CCOCC4)C(C5=C(C2=O)C6=C(N5)C=C(C=C6)C#N)(C)C
保管

In vitro
Batch:

DMSO : 7 mg/mL ( (14.5 mM)； Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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