Alectinib (CH5424802)

For research use only. Not for use in humans.

製品コードS2762 別名：AF-802,RG-7853

Alectinib (CH5424802)化学構造

CAS No. 1256580-46-7

Alectinib (CH5424802, AF-802, RG-7853) 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.

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文献中Selleckの製品使用例(49)

製品安全説明書

ALK阻害剤の選択性比較

生物活性

製品説明 Alectinib (CH5424802, AF-802, RG-7853) 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.
ターゲット
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
体外試験

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]
細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H2228 MWfLbY5ie2ViYYPzZZk> M1nufp4yKM7:TR?= NXSwNI1ZeHKndnXueJMh[XW2b4Doc5NxcG:{eXzheIlwdiCxZjDBUGs> NUnZO|BCOjF3N{W4OlY>
KARPAS-299 NFrGN|NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVT1e2ZlhjFyIN88US=> NGT1eohKSzVyPUOgcm0> NVLkbmEyOjF3N{W4OlY>
SR M2PheGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4npTJ4yOCEQvF2= NGrCelVKSzVyPU[uPUBvVQ>? NIHMUoozOTV5NUi2Oi=>
HDLM-2 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUPGXGJjhjFyIN88US=> MWPJR|UxRjFyLECwNEBvVQ>? NXGzWoh6OjF3N{W4OlY>
NB-1 M1ryfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M37Q[J4yOCEQvF2= MknJTWM2OD12LkWgcm0> NVfHcFNQOjF3N{W4OlY>
KELLY NXXCT3Q2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4LRc54yOCEQvF2= NHHFNohKSzVyPU[yJI5O Mlf5NlE2PzV6Nk[=
SK-N-FI NFLkOVVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEO0R2J,OTBizszN MmXtTWM2OD5zMDywNFAhdk1? NXf1Tox2OjF3N{W4OlY>
NCI-H2228 NWHXVIFrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3PS[54yOCEQvF2= M4S2RWlEPTB;NUOgcm0> MXSyNVU4PTh4Nh?=
Calu-3 NETkTGFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlrVglExKM7:TR?= M37kb2lEPTB;PkGwMFAxOCCwTR?= NVHiWJlZOjF3N{W4OlY>
PC-1 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGnrUGJ,OTBizszN NIGzfnZKSzVyPkGwMFAxOCCwTR?= NIrEWZEzOTV5NUi2Oi=>
NCI-H23 NHuxSZpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWL+NVAh|ryP NXPhTZh2UUN3ME2zOlAxKG6P M2GxNlIyPTd3OE[2
Calu-1 MkT4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXTzWpB[hjFyIN88US=> NFT5cnpKSzVyPkGwMFAxOCCwTR?= M{HNblIyPTd3OE[2
NCI-H2009 M1nwRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoK2glExKM7:TR?= MULJR|UxRjFyLECwNEBvVQ>? MWWyNVU4PTh4Nh?=
NCI-H1993 M1GyWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MojaglExKM7:TR?= NWLZbIdJUUN3ME6xNEwxODBibl2= NVjqdVZCOjF3N{W4OlY>
MKN-45 NYjkV5MzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NELNTop,OTBizszN MUDJR|UxRjFyLECwNEBvVQ>? NET4UpkzOTV5NUi2Oi=>
SNU-5 NX[xbmxQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{j0dp4yOCEQvF2= NEH0S5FKSzVyPUG4NFAhdk1? MlP6NlE2PzV6Nk[=
KATO-III M4jBNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1f5UZ4yOCEQvF2= NV7sUmlyUUN3ME23PVAxKG6P NFXkcpczOTV5NUi2Oi=>
SK-BR-3 NIiyTo5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NULqOYJUhjFyIN88US=> MlG0TWM2OD5zMDywNFAhdk1? M1XKSlIyPTd3OE[2
BT-483 NXriSoFWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXe0d4I{hjFyIN88US=> MlryTWM2OD5zMDywNFAhdk1? MX2yNVU4PTh4Nh?=
PC-3 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWjOPYJ3hjFyIN88US=> MmnOTWM2OD5zMDywNFAhdk1? MW[yNVU4PTh4Nh?=
22Rv1 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUSyUYtYhjFyIN88US=> MWLJR|UxRjFyLECwNEBvVQ>? NXy4TYk{OjF3N{W4OlY>
U-87 MG M{LwO2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3HVZ54yOCEQvF2= NWjPblZTUUN3ME6xNEwxODBibl2= NWW0U3B2OjF3N{W4OlY>
H3122 NYDxV|Z4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{H0OZ4yOCEQvF2= M37BXGlEPTB;M{Ogcm0> NYqwfpBxOjVyOU[0NFA>
LC-2/ad MX\BdI9xfG:|aYOgZZN{[Xl? M{ToRZ4yKM7:TR?= NHvqWFdFVVOR Mki0bY5lfWOnczDhdI9xfG:|aYO= NXjaPZpYOjV|NEmzNFc>
LC-2/ad NHPpZnJHfW6ldHnvckBie3OjeR?= M1e3NJ4yKM7:TR?= M3zOO2ROW09? MlfabY5pcWKrdIOgeIhmKE2DUFugd4lodmGuaX7nJJBifGi5YYm= MXSyOVM1QTNyNx?=
Ba/F3 MWrGeY5kfGmxbjDhd5NigQ>? MUX+NUDPxE1? NXvKS5BjTE2VTx?= MnHUd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YhTVKNIHHu[EBqdmO{ZXHz[ZMhfGinIHHieY5l[W6lZTDv[kBDUU1? MnP6NlU{PDl|MEe=
SNU-2535 NWrnRmhJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Moq4glExKM7:TR?= M1fxfGlEPTB;M{OuNUBvVQ>? NWnNcoF1OjZ6NEm2N|c>
SNU-2535 MkfDT4lv[XOnIHHzd4F6 Mlq2glEh|ryP MXPpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGOSzDhcoQhcXS|IHTve45{fHKnYX2gcY9t\WO3bHXzJGVTUzFxMjDhcoQhSUuW M2XtT|I3QDR7NkO3

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アッセイ
Methods Test Index PMID
Western blot
pALK / ALK / pAKT / AKT / pERK / ERK / pS6 / S6 ; 

PubMed: 25228534     


Parental H3122 and CHR-A1 cells were treated with alectinib at the indicated concentrations for 6 hrs. Cell extracts were immunoblotted to detect the indicated proteins.

PARP / cleaved PARP / Akt / caspase 3 / Cleaved caspase 3; 

PubMed: 28455243     


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 were treated with 10 μM alectinib for various time points as indicated. The anti-β-Actin antibody was used as a loading c䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ

pROS1 / ROS1 / pSTAT3 / STAT3; 

PubMed: 25351743     


Inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74-ROS1 expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, or ASP3026 for 3 h. Cell lysates were immunoblotted to detect the indicated䲧疝Ỵ疞㧀

p-EGFR Tyr1068 / EGFR / p-HER3 Tyr1222 / HER3 / p-IGF-1R Tyr1135 / IGF-1R; 

PubMed: 26992917     


Cells were treated with indicated drugs for 1 hour; immunoblotting for RTKs in both resistant cell lines showed upregulation of phosphor-EGFR and phosphor-HER3 when compared with parental cells.

25228534 28455243 25351743 26992917
Growth inhibition assay
Cell viability ; 

PubMed: 25228534     


(A) Cells were seeded in 96-well black plates and treated with increasing concentrations of alectinib for 72 hrs. Cell survival was analyzed using the CellTiter-Glo assay. While H3122 cells showed high sensitivity to alectinib (red line), H3122 CHR-A1 cel䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෋à鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼瘿⟸෕ᾰƌ

25228534
体内試験 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]

お薦めの試験操作（参考用のみ）

キナーゼ試験：[1]
- 合併

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.
細胞試験： [1]
- 合併
  • 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.
    (参考用のみ)
動物試験：[1]
- 合併
  • 動物モデル： SCID or nude mice bearing NCI-H2228
  • 投薬量： 20 mg/kg
  • 投与方法： Oral administration
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 0.5 mg/mL (1.03 mM) warming
Water Insoluble
Ethanol Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 482.62
化学式

C30H34N4O2
CAS No. 1256580-46-7
Storage powder
in solvent
別名 AF-802,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

投与溶媒組成計算器(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）
投与量 mg/kg 動物平均体重 g 投与体積（動物毎） ul 動物数 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
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA（製品ページで利用可能な）。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：

総分子量：g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04644315 Not yet recruiting Drug: Alectinib Solid Tumors Hoffmann-La Roche January 4 2021 Phase 2
NCT04111705 Recruiting Drug: Lorlatinib Non Small Cell Lung Cancer Metastatic Intergroupe Francophone de Cancerologie Thoracique August 5 2020 Phase 2
NCT03445000 Recruiting Drug: Alectinib Non-small Cell Lung Cancer|Non-small Cell Lung Cancer Metastatic|Non-small Cell Lung Cancer Recurrent European Thoracic Oncology Platform|Hoffmann-La Roche November 6 2018 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須
selleck catalog

ALKシグナル伝達経路

ALK Inhibitors with Unique Features

  • Non-specific ALK Inhibitor

    GSK1838705A : IGF-1R, IC50=2.0 nM; IR, IC50=1.6 nM, ALK, IC50=0.5 nM.

  • Most Potent ALK Inhibitor

    Ceritinib (LDK378) : ALK, IC50=0.2 nM.

  • FDA-approved ALK Inhibitor

    Crizotinib (PF-02341066) : Approved by FDA for non-small cell lung carcinoma (NSCLC).

  • Newest ALK Inhibitor

    ASP3026 New : Novel and selective inhibitor for ALK with IC50 of 3.5 nM.

相関ALK製品

  • Lorlatinib (PF-6463922)

    Lorlatinib (PF-6463922) is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. PF-06463922 induces apoptosis. Phase 1.

  • Erlotinib

    Erlotinib (CP358774, NSC 718781) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.

  • Bemcentinib (R428)

    Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

  • TAE684 (NVP-TAE684)

    TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.

  • GSK1838705A

    GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.

    Features:A small-molecule kinase inhibitor of IGF-1R and the insulin receptor.

  • AP26113-analog (ALK-IN-1)

    AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.

    Features:At least 10-fold more potent and selective in ALK inhibition relative to crizotinib.

  • ASP3026

    ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.

Tags: Alectinib (CH5424802)を買う | Alectinib (CH5424802) ic50 | Alectinib (CH5424802)供給者 | Alectinib (CH5424802)を購入する | Alectinib (CH5424802)費用 | Alectinib (CH5424802)生産者 | オーダーAlectinib (CH5424802) | Alectinib (CH5424802)化学構造 | Alectinib (CH5424802)分子量 | Alectinib (CH5424802)代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID