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.

Size Price Stock Quantity  
USD 170 In stock
USD 270 In stock
USD 770 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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.

Purity & Quality Control

Choose Selective ALK Inhibitors

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.
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 MkHLT4lv[XOnIHHzd4F6 MljDglEh|ryP MYTwdoV3\W62czDheZRweGixc4Doc5J6dGG2aX;uJI9nKEGOSx?= M2nJblIyPTd3OE[2
KARPAS-299 M2P5TWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHTwUY5,OTBizszN M1jiWmlEPTB;MzDuUS=> NGjUN4MzOTV5NUi2Oi=>
HDLM-2 NFLmUWRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1j3XZ4yOCEQvF2= NYjMUlFRUUN3ME6xNEwxODBibl2= NULCc3hXOjF3N{W4OlY>
NB-1 MmDCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIHuXmV,OTBizszN NF\3R5dKSzVyPUSuOUBvVQ>? M1\SU|IyPTd3OE[2
KELLY NY\oU4I4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWn+NVAh|ryP NFPF[WdKSzVyPU[yJI5O M3zHTlIyPTd3OE[2
SK-N-FI Mk\OS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUnVNZZihjFyIN88US=> NV7vO2RtUUN3ME6xNEwxODBibl2= MYKyNVU4PTh4Nh?=
NCI-H2228 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml3kglExKM7:TR?= MUjJR|UxRTV|IH7N NWKzb25JOjF3N{W4OlY>
Calu-3 NWHGPG12T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1vK[p4yOCEQvF2= MVfJR|UxRT5zMDywNFAhdk1? M33a[VIyPTd3OE[2
PC-1 NGW2XHZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV36eI9ChjFyIN88US=> NIPUPHVKSzVyPkGwMFAxOCCwTR?= MmOzNlE2PzV6Nk[=
NCI-H23 NI\QTnJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{jRb54yOCEQvF2= NWfZRVNCUUN3ME2zOlAxKG6P NF:4PYEzOTV5NUi2Oi=>
Calu-1 NXXIfJVmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXH+NVAh|ryP NFTlO2NKSzVyPkGwMFAxOCCwTR?= M3zifFIyPTd3OE[2
NCI-H2009 M{D6VWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml:4glExKM7:TR?= Ml;jTWM2OD5zMDywNFAhdk1? MXuyNVU4PTh4Nh?=
NCI-H1993 NYrTVHE5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2Tw[J4yOCEQvF2= NWHs[5F{UUN3ME6xNEwxODBibl2= MmezNlE2PzV6Nk[=
MKN-45 MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3TGfZ4yOCEQvF2= MUDJR|UxRjFyLECwNEBvVQ>? M{TkZlIyPTd3OE[2
SNU-5 MoftS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3jQ[Z4yOCEQvF2= NEjiRXdKSzVyPUG4NFAhdk1? MUCyNVU4PTh4Nh?=
KATO-III MmmxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MW\+NVAh|ryP NUDS[lhyUUN3ME23PVAxKG6P MYCyNVU4PTh4Nh?=
SK-BR-3 MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWO2[mtkhjFyIN88US=> M4fjU2lEPTB-MUCsNFAxKG6P Mo\INlE2PzV6Nk[=
BT-483 NUXsV|lLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF;UPWJ,OTBizszN MVrJR|UxRjFyLECwNEBvVQ>? NEXz[nczOTV5NUi2Oi=>
PC-3 NF\iVIxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkfHglExKM7:TR?= NHm0[FFKSzVyPkGwMFAxOCCwTR?= NEe5OlYzOTV5NUi2Oi=>
22Rv1 MkKxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnTmglExKM7:TR?= NIG0RmlKSzVyPkGwMFAxOCCwTR?= M4foNFIyPTd3OE[2
U-87 MG NGjYV|ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYf+NVAh|ryP NILSdYJKSzVyPkGwMFAxOCCwTR?= NXK1VnByOjF3N{W4OlY>
H3122 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlrrglExKM7:TR?= MlfBTWM2OD1|MzDuUS=> NUDBd|d7OjVyOU[0NFA>
LC-2/ad Ml\PRZBweHSxc3nzJIF{e2G7 MnTnglEh|ryP NYTZTmVVTE2VTx?= M3rSTYlv\HWlZYOgZZBweHSxc3nz M4nUR|I2OzR7M{C3
LC-2/ad MkjMSpVv[3Srb36gZZN{[Xl? MnLIglEh|ryP M3\UfGROW09? MnXMbY5pcWKrdIOgeIhmKE2DUFugd4lodmGuaX7nJJBifGi5YYm= NV3nPY5KOjV|NEmzNFc>
Ba/F3 NI[2[nVHfW6ldHnvckBie3OjeR?= MoDnglEh|ryP NUXuelZPTE2VTx?= NF\NcXB{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCHUlugZY5lKGmwY4LlZZNmeyC2aHWgZYJ2dmSjbnPlJI9nKEKLTR?= MlTGNlU{PDl|MEe=
SNU-2535 M{nnPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWP+NVAh|ryP NG[1WFNKSzVyPUOzMlEhdk1? M3[z[FI3QDR7NkO3
SNU-2535 M2TYcmtqdmG|ZTDhd5NigQ>? M3nCVZ4yKM7:TR?= M2TpfYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVzLJIFv\CCrdIOg[I94dnO2cnXhcUBud2ynY4Xs[ZMhTVKNMT:yJIFv\CCDS2S= NH25U5EzPjh2OU[zOy=>

... 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]


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


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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

ALK Signaling Pathway Map

ALK Inhibitors with Unique Features

Related ALK Products4

Tags: buy Alectinib (CH5424802) | Alectinib (CH5424802) supplier | purchase Alectinib (CH5424802) | Alectinib (CH5424802) cost | Alectinib (CH5424802) manufacturer | order Alectinib (CH5424802) | Alectinib (CH5424802) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID