Alectinib (CH5424802)

Catalog No.S2762 Synonyms: AF-802,RG-7853

Alectinib (CH5424802) Chemical Structure

Molecular Weight(MW): 482.62

Alectinib (CH5424802) 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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4 Customer Reviews

  • Immunoblot analysis of full-length DCTN1-ALK proteins. An expression vector encoding DCTN1-ALK cDNA was introduced into H1299 lung cancer cells, which do not express endogenous ALK. The transfectants were then exposed to crizotinib and alectinib. Levels of phosphorylation at tyrosine 1604 were determined 24 hours after treatment with 0, 0.2, 1.0, or 5.0 μM of each drug.

    Oncologist, 2017, 22(2):158-164. Alectinib (CH5424802) purchased from Selleck.

    Sensitivity of the H3122 cell line to ALK inhibitors (crizotinib and alectinib). To examine the sensitivity of ALK inhibitors, used an MTT assay. The experiment was performed in triplicate. (A) Growth inhibitory effect of crizotinib. The H3122 cell line was sensitive to crizotinib under a normoxic state, compared with a hypoxic state. The graphs, mean of independent triplicate experiments; error bars, SD. (B) IC50 of ALK inhibitors. The IC50 values of both inhibitors in the H3122 cell lines were significantly higher under hypoxia than under normoxia (crizotinib, *P=0.028 and alectinib, *P=0.0035). *P<0.05.

    Int J Oncol 2014 45(4), 1430-6. Alectinib (CH5424802) purchased from Selleck.

  • Western blotting data of NPM/ALK-transformed BaF3 cells, both wild-type and L1196M-mutant, treated with CH5424802 for 4 hours. The blot shows phospho-ALK signal (Y1604), as an indicator of NPM/ALK activation.

    Prof. Gambacorti from Università degli Studi di Milano Bicocc. Alectinib (CH5424802) purchased from Selleck.

    Cell growth data, performed by tritiated thymidine uptake assay, using NPM/ALK wild-type -transformed BaF3 cells.CH5424802 demonstrated a very good ability to block NPM/ALK-transformed BaF3 cells proliferation with an IC50 of 3 nM.

    Prof. Gambacorti from Università degli Studi di Milano Bicocc. Alectinib (CH5424802) purchased from Selleck.

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Biological Activity

Description Alectinib (CH5424802) 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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H2228 MnPFT4lv[XOnIHHzd4F6 M3e5TJ4yKM7:TR?= NFX3fo1xemW4ZX70d{BifXSxcHjvd5Bpd3K7bHH0bY9vKG:oIFHMTy=> MoXuNlE2PzV6Nk[=
KARPAS-299 NV3Lc2FLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn:wglExKM7:TR?= MXHJR|UxRTNibl2= NWfzO3VXOjF3N{W4OlY>
SR NITMNpVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVf+NVAh|ryP MofHTWM2OD14Lkmgcm0> M2XkbFIyPTd3OE[2
HDLM-2 NUjTUlFKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlnhglExKM7:TR?= Mn\PTWM2OD5zMDywNFAhdk1? NYLRRZpVOjF3N{W4OlY>
NB-1 NFvNc5JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHzYTpp,OTBizszN M1\aR2lEPTB;ND61JI5O M1LCT|IyPTd3OE[2
KELLY M3fhZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHKxNoh,OTBizszN M4DHSGlEPTB;NkKgcm0> NGnYcmkzOTV5NUi2Oi=>
SK-N-FI NWXlSGFGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3;VTJ4yOCEQvF2= MnrMTWM2OD5zMDywNFAhdk1? NEnIbYEzOTV5NUi2Oi=>
NCI-H2228 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIrHPZF,OTBizszN M1zDZ2lEPTB;NUOgcm0> NIT5b5IzOTV5NUi2Oi=>
Calu-3 NHzxO4ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkixglExKM7:TR?= MVrJR|UxRT5zMDywNFAhdk1? NYnpOpdiOjF3N{W4OlY>
PC-1 M{XFWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV;+NVAh|ryP NYXURoNMUUN3ME6xNEwxODBibl2= M1\5R|IyPTd3OE[2
NCI-H23 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mmm2glExKM7:TR?= NWnVXGdEUUN3ME2zOlAxKG6P M1LmUFIyPTd3OE[2
Calu-1 MkfZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVrtcm4yhjFyIN88US=> Ml7RTWM2OD5zMDywNFAhdk1? MUeyNVU4PTh4Nh?=
NCI-H2009 MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUP+NVAh|ryP NIrJTXpKSzVyPkGwMFAxOCCwTR?= NXu4XpEzOjF3N{W4OlY>
NCI-H1993 NXyxOFNkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2TXXZ4yOCEQvF2= NHTqTpJKSzVyPkGwMFAxOCCwTR?= MkD3NlE2PzV6Nk[=
MKN-45 NXTjdoxrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{DKWp4yOCEQvF2= MWfJR|UxRjFyLECwNEBvVQ>? Mny3NlE2PzV6Nk[=
SNU-5 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkLaglExKM7:TR?= M2nNVGlEPTB;MUiwNEBvVQ>? M2LYOVIyPTd3OE[2
KATO-III NI[0N|FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NELnNmV,OTBizszN NYK5[oFWUUN3ME23PVAxKG6P MWeyNVU4PTh4Nh?=
SK-BR-3 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEjn[25,OTBizszN MVvJR|UxRjFyLECwNEBvVQ>? NELTdG0zOTV5NUi2Oi=>
BT-483 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHT2[2t,OTBizszN NUjQeVd7UUN3ME6xNEwxODBibl2= NYr6WlB6OjF3N{W4OlY>
PC-3 NXraWlFZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2\3S54yOCEQvF2= M4LCe2lEPTB-MUCsNFAxKG6P MlfXNlE2PzV6Nk[=
22Rv1 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYLwVVF5hjFyIN88US=> MUTJR|UxRjFyLECwNEBvVQ>? NFjwNZUzOTV5NUi2Oi=>
U-87 MG NUHwUo1bT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIXVcph,OTBizszN NXrSWpAzUUN3ME6xNEwxODBibl2= MmnQNlE2PzV6Nk[=
H3122 MoHvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M325WJ4yOCEQvF2= NXTnd4p2UUN3ME2zN{BvVQ>? MXKyOVA6PjRyMB?=
LC-2/ad NFnPSZdCeG:ydH;zbZMh[XO|YYm= M2Ky[Z4yKM7:TR?= M1nkU2ROW09? MYHpcoR2[2W|IHHwc5B1d3Orcx?= MWSyOVM1QTNyNx?=
LC-2/ad M3;RfmZ2dmO2aX;uJIF{e2G7 M2HSUp4yKM7:TR?= M2jSV2ROW09? M2eyWYlvcGmkaYTzJJRp\SCPQWDLJJNq\26jbHnu[{Bx[XSqd3H5 M{nZdFI2OzR7M{C3
Ba/F3 MlLmSpVv[3Srb36gZZN{[Xl? M1e1bJ4yKM7:TR?= MWXEUXNQ NH;XWWR{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCHUlugZY5lKGmwY4LlZZNmeyC2aHWgZYJ2dmSjbnPlJI9nKEKLTR?= MW[yOVM1QTNyNx?=
SNU-2535 MYjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWnubHg6hjFyIN88US=> MXvJR|UxRTN|LkGgcm0> MUiyOlg1QTZ|Nx?=
SNU-2535 MojJT4lv[XOnIHHzd4F6 NYLBcmkyhjFizszN M{PDbYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVzLJIFv\CCrdIOg[I94dnO2cnXhcUBud2ynY4Xs[ZMhTVKNMT:yJIFv\CCDS2S= MoO1NlY5PDl4M{e=

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[1]
+ Expand
  • Cell lines: NSCLC, A549 and HCC827 cell lines
  • Concentrations: 0-1 μM
  • Incubation Time: 5 days
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: SCID or nude mice bearing NCI-H2228
  • Formulation: 0.02 N HCl, 10% DMSO, 10% Cremophor EL, 15% PEG400, and 15% HPCD (2-hydroxypropyl-β-cyclodextrin)
  • Dosages: 20 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 0.5 mg/mL warmed (1.03 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 482.62
Formula

C30H34N4O2

CAS No. 1256580-46-7
Storage powder
in solvent
Synonyms AF-802,RG-7853

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03737994 Not yet recruiting ALK Gene Rearrangement|ALK Positive|Non-Squamous Non-Small Cell Lung Carcinoma|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8 National Cancer Institute (NCI) January 13 2019 Phase 2
NCT03596866 Not yet recruiting ALK-positive Advanced NSCLC Ariad Pharmaceuticals|Takeda December 15 2018 Phase 3
NCT03445000 Recruiting 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
NCT03546894 Recruiting Anaplastic Lymphoma Kinase-positive|Carcinoma Non-small-cell Lung Millennium Pharmaceuticals Inc.|Takeda July 23 2018 --
NCT03498521 Recruiting Cancer of Unknown Primary Site Hoffmann-La Roche|Foundation Medicine Inc. July 10 2018 Phase 2
NCT03158389 Recruiting Glioblastoma Adult University Hospital Heidelberg|German Cancer Aid|German Cancer Research Center|National Center for Tumor Diseases Heidelberg May 7 2018 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID