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CO-1686 (AVL-301)

EGFR inhibitor CAS# 1374640-70-6

CO-1686 (AVL-301)

Catalog No. BCC1490----Order now to get a substantial discount!

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Quality Control of CO-1686 (AVL-301)

Quality Control & MSDS

Number of papers citing our products

Chemical structure

CO-1686 (AVL-301)

3D structure

Chemical Properties of CO-1686 (AVL-301)

Cas No. 1374640-70-6 SDF Download SDF
PubChem ID 57335384 Appearance Powder
Formula C27H28F3N7O3 M.Wt 555.55
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Rociletinib; AVL-301; CNX-419
Solubility DMSO : ≥ 43 mg/mL (77.40 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
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
Standard InChIKey HUFOZJXAKZVRNJ-UHFFFAOYSA-N
Standard InChI InChI=1S/C27H28F3N7O3/c1-4-24(39)32-18-6-5-7-19(14-18)33-25-21(27(28,29)30)16-31-26(35-25)34-22-9-8-20(15-23(22)40-3)37-12-10-36(11-13-37)17(2)38/h4-9,14-16H,1,10-13H2,2-3H3,(H,32,39)(H2,31,33,34,35)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CO-1686 (AVL-301)

DescriptionCO-1686 is an irreversible and orally delivered inhibitor of EGFR with IC50 values of 21.5 nM and 303.3 nM for L858R/T790M mutant EGFR and wild-type EGFR, respectively.
TargetsL858R/T790M mutant EGFRwild-type EGFR    
IC5021.5 nM303.3 nM    

Protocol

Cell Assay [1]
Cells are seeded at 3,000 cells/well in growth media supplemented with 5% FBS, 2 mM L-glutamine, and 1 % P/S, allowed to adhere overnight, and treated with a dilution series of test compound (CO-1686) for 72 hr. Cell viability is determined by CellTiter Glo and results are represented as background-subtracted relative light units normalized to a DMSO-treated control. Growth inhibition (GI50) values are determined by GraphPad Prism 5.04. Combination index (CI) data is generated using CalcuSyn.

Animal Administration [1]
Briefly, NCr nu/nu mice are sub-cutaneously implanted with 1×107 tumor cells in 50% Matrigel (injection volume of 0.2 mL/mouse). Once tumors reached 100-200 mm3, Animals are dosed with compounds (CO-1686) as outlined (N=10 animals/gp). Briefly, LUM1686 PDX tumor fragments, harvested from donor mice, are inoculated into BALB/c nude mice. Administration of test compounds (CO-1686) is initiated at a mean tumor size of approximately 160 mm3. Tumor growth is monitored over time to determine tumor growth inhibition of the experimental agent vs. vehicle. The endpoint of the experiment is a mean tumor volume (MTV) in control group of 2000 mm3. Percent TGI is defined as the difference between the MTV of the designated control group and the MTV of the drug-treated group, expressed as a percentage of the MTV of the designated control group. Data is presented as mean±standard error of the mean (SEM).

References:
[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25.

CO-1686 (AVL-301) Dilution Calculator

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Preparing Stock Solutions of CO-1686 (AVL-301)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.8 mL 9.0001 mL 18.0002 mL 36.0004 mL 45.0005 mL
5 mM 0.36 mL 1.8 mL 3.6 mL 7.2001 mL 9.0001 mL
10 mM 0.18 mL 0.9 mL 1.8 mL 3.6 mL 4.5 mL
50 mM 0.036 mL 0.18 mL 0.36 mL 0.72 mL 0.9 mL
100 mM 0.018 mL 0.09 mL 0.18 mL 0.36 mL 0.45 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CO-1686 (AVL-301)

CO-1686 is an irreversible and orally delivered inhibitor of mutant EGFR with IC50 value of < 0.51 nM for recombinant EGFR L858R/T790M [1].

CO-1686 covalently modified Cys797 in the ATP binding pocket of the EGFR kinase. It also modified this residue in the EGFR L858R/T790M kinase domain. In the in vitro assay, CO-1686 potently inhibited EGFR L858R/T790M kinase with about 22-fold selectivity over wild-type EGFR. Among the 23 targets treated with CO-1686, EGFR del19, T790M, L858R/T790M and L858R mutants demonstrated the highest inhibition degree. In 4 NSCLC cell lines expressing mutant EGFR (HCC827, PC9, HCC827-EPR and NCI-H1975), CO-1686 potently inhibited cell proliferation with GI50 values of 7-32 nM. CO-1686 also inhibited some minor EGFR mutants including G719S, the exon 19 insertion and L861Q. In mice with NCI-H1975 xenografts, 100 mg/kg/day administration of CO-1686 caused tumor regressions [2].

References:
[1] Walter A O, Tjin R, Haringsma H, et al. CO-1686, an orally available, mutant-selective inhibitor of the epidermal growth factor receptor (EGFR), causes tumor shrinkage in Non-Small Cell Lung Cancer (NSCLC) with T790M resistance mutations. Mol Cancer Ther, 2011, 10(11 Suppl).
[2] Walter A O, Sjin R T T, Haringsma H J. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.

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Description

Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

Keywords:

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