Rociletinib (CO-1686)

For research use only.

Catalog No.S7284 Synonyms: AVL-301

28 publications

Rociletinib (CO-1686) Chemical Structure

CAS No. 1374640-70-6

Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.

Size Price Stock Quantity  
EUR 291 In stock
EUR 953 In stock
Bulk Discount

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

Selleck's Rociletinib (CO-1686) has been cited by 28 publications

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.
EGFR (L858R/T790M) [1]
(Cell-free assay)
EGFR (wt) [1]
(Cell-free assay)
21.5 nM(Ki) 303.3 nM(Ki)
In vitro

CO-1686 inhibits p-EGFR with IC50 ranging from 62 to 187 nM in the mutant EGFR–expressing cells, while inhibits EGFR phosphorylation with IC50 of > 2,000 nM in the three WT EGFR–expressing cells. CO-1686 selectively inhibits growth of NSCLC cells expressing mutant EGFR with GI50 ranging from 7 to 32 nM, and induces apoptosis. CO-1686–resistant NSCLC cell lines exhibits signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1975 MYHLbY5ie2ViYYPzZZk> MlrkglUh|ryP Mn[wSG1UVw>? Ml\VbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJFYzKG6P MWOyOFA3PTd|MR?=
HCC827-EPR NYr1bVlXU2mwYYPlJIF{e2G7 MlT4glUh|ryP M13LZ2ROW09? M4PJWYlvcGmkaYTzJJBGT0[UIIfpeIghUUN3MDDv[kAyQDBibl2= MkCyNlQxPjV5M{G=
A431 MYLLbY5ie2ViYYPzZZk> MnzKglUh|ryP NIrmfWNFVVOR NIf5UYVqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjR|M{Ggcm0> MmXuNlQxPjV5M{G=
NCI-H1299 MkO1T4lv[XOnIHHzd4F6 Ml\6glUh|ryP MlrmSG1UVw>? MnTpbY5pcWKrdIOgdGVITlJid3n0bEBKSzVyIH;mJF4zODByIH7N M2[4dlI1ODZ3N{Ox
NCI-H358 MlHtT4lv[XOnIHHzd4F6 MUT+OUDPxE1? M33IT2ROW09? NFnQ[|NqdmirYnn0d{BxTUeIUjD3bZRpKEmFNUCgc4YhRjJyMECgcm0> NFTFdWUzPDB4NUezNS=>
NCI-H1975 NF3JNlZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGn2PIV,PSEQvF2= NXi3eINVTE2VTx?= M4\iVmdKPTB;M{Kgcm0> MnL1NlQxPjV5M{G=
HCC827 NUHHRo5QT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1i1Wp42KM7:TR?= Mo\SSG1UVw>? MoWzS2k2OD15IH7N MXuyOFA3PTd|MR?=
PC9 NV2wOVFlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1vKcJ42KM7:TR?= NYrFOYtRTE2VTx?= MX;HTVUxRTJ4IH7N MlrZNlQxPjV5M{G=
A431 MmLHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFf6NIt,PSEQvF2= Mk\nSG1UVw>? MYDHTVUxRTV2NzDuUS=> NYDpWFdCOjRyNkW3N|E>
NCI-H1299 M3nreGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3nhNp42KM7:TR?= MXjEUXNQ NVWyNlhlT0l3ME20Nlc2KG6P M3jkb|I1ODZ3N{Ox
NCI-H358 MlLLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mo\EglUh|ryP MWXEUXNQ MorIS2k2OD1zOEC2JI5O NX\uNpJTOjRyNkW3N|E>
PC-9 (exon 19del) NHf2O3BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUf+NVAh|ryP MmT2SG1UVw>? NYrTRW1YUUN3ME24OEBvVQ>? NXXnPYRVOjZ3MUW0OlQ>
H3255 (L858R) NF3RXIVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2LiOp4yOCEQvF2= MlXrSG1UVw>? MlvaTWM2OD1|NTDuUS=> MkfGNlY2OTV2NkS=
PC-9ER (exon 19del+T790M) MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWj+NVAh|ryP Mk\hSG1UVw>? M{nnUWlEPTB;M{egcm0> MV:yOlUyPTR4NB?=
H1975 (L858R+T790M) MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXjVOXREhjFyIN88US=> Ml;ZSG1UVw>? MW\JR|UxRTJ|IH7N NY[xbmFNOjZ3MUW0OlQ>
BID007 (A763_Y764insFQEA) MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{\q[Z4yOCEQvF2= MVfEUXNQ M1nT[2lEPTB;MUK3PEBvVQ>? NHLSe|AzPjVzNUS2OC=>
Ba/F3 (FQEA) Mom4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVT0Vpl5hjFyIN88US=> NW\iRmZ6TE2VTx?= M{T1RmlEPTB;NkezJI5O MlXQNlY2OTV2NkS=
Ba/F3 (HH) NFrs[YdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M13heZ4yOCEQvF2= NFnxboJFVVOR NVS2S3FPUUN3ME2xO|MxKG6P NUjDN4FwOjZ3MUW0OlQ>
Ba/F3 (ASV) M1PF[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3fIdp4yOCEQvF2= MoTnSG1UVw>? M{jmW2lEPTB;NUK5NEBvVQ>? NGS4d5kzPjVzNUS2OC=>

... Click to View More Cell Line Experimental Data

In vivo CO-1686 causes dose-dependent and significant tumor growth inhibition in all EGFR-mutant models as well as human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice. [1]


Kinase Assay:[1]
- Collapse

Inhibition Kinetics Studies:

Recombinant human wild-type and T790M/L858R double mutant EGFR, both Nterminal GST-tagged, are used in the assay. The Omnia continuous read assay is performed as described by the vendor.
Cell Research:[1]
- Collapse
  • Cell lines: NSCLC cell lines expressing mutant EGFR (HCC827, PC9, HCC827-EPR, and NCI-H1975) and cell lines expressing WT EGFR (A431, NCI-H1299, and NCI-H358)
  • Concentrations: ~10 μM
  • Incubation Time: 72 hours
  • Method: Cells are seeded at 3,000 cells per well in growth media supplemented with 5% FBS, 2 mmol/L, L-glutamine, and 1% penicillin–streptomycin, allowed to adhere overnight, and treated with a dilution series of test compounds for 72 hours. Cell viability is determined by CellTiter-Glo, and results are represented as background-subtracted relative light units normalized to a dimethyl sulfoxide (DMSO)–treated control. Growth inhibition (GI 50) values are determined by GraphPad Prism 5.04. MK-2206 and XL-880 compounds are obtained from Selleck Chemical. CI data are generated using CalcuSyn.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice.
  • Dosages: ~50 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (180.0 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
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 555.55


CAS No. 1374640-70-6
Storage powder
in solvent
Synonyms AVL-301
Smiles CC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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 (mg) = Concentration (mM) × Volume (mL) × 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

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

EGFR Signaling Pathway Map

Related EGFR Products

Tags: buy Rociletinib (CO-1686) | Rociletinib (CO-1686) supplier | purchase Rociletinib (CO-1686) | Rociletinib (CO-1686) cost | Rociletinib (CO-1686) manufacturer | order Rociletinib (CO-1686) | Rociletinib (CO-1686) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID