Anti-cancer drugs Biological activity In vitro study In vivo studies Synthesis method
ChemicalBook > CAS DataBase List > CO-1686

CO-1686

Anti-cancer drugs Biological activity In vitro study In vivo studies Synthesis method
Product Name
CO-1686
CAS No.
1374640-70-6
Chemical Name
CO-1686
Synonyms
CS-851;CNX-419;AVL-301;CO-1686;ROCILETINIB;Pyridostadin;Clovis CO-1686;CO-1686/CO1686;CO-1686, >=98%;CO-1686 (AVL-301)
CBNumber
CB22666396
Molecular Formula
C27H28F3N7O3
Formula Weight
555.55
MOL File
1374640-70-6.mol
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CO-1686 Property

Melting point:
202 - 205°C (dec.)
Density 
1.372±0.06 g/cm3(Predicted)
storage temp. 
Amber Vial, -20°C Freezer, Under inert atmosphere
solubility 
DMSO (Slightly), Methanol (Slightly)
form 
Solid
pka
13.23±0.70(Predicted)
color 
Off-White
CAS DataBase Reference
1374640-70-6
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Safety

Risk Statements 
23-25-36
Safety Statements 
24
HS Code 
29335990
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
16244
Product name
CO-1686
Purity
≥98%
Packaging
1mg
Price
$68
Updated
2024/03/01
Cayman Chemical
Product number
16244
Product name
CO-1686
Purity
≥98%
Packaging
5mg
Price
$201
Updated
2024/03/01
Cayman Chemical
Product number
16244
Product name
CO-1686
Purity
≥98%
Packaging
10mg
Price
$335
Updated
2024/03/01
TRC
Product number
C633000
Product name
CO1686
Packaging
100mg
Price
$275
Updated
2021/12/16
ChemScene
Product number
CS-1631
Product name
Rociletinib
Purity
99.59%
Packaging
100mg
Price
$250
Updated
2021/12/16
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CO-1686 Chemical Properties,Usage,Production

Anti-cancer drugs

On May 20, 2014, Clovis Oncology announced that the US FDA had granted its test drug CO-1686 for breakthrough treatment drug qualification, as a second line, single administrated drug for the treatment of EFGR mutation non-small cell lung cancer (NSCLC) of the T790M mutation patients. The awarding for this breakthrough therapeutic drug eligibility was based on the efficacy and safety results of Co-1686 in an ongoing Phase 1/2 study. Data of related study have shown that CO-1686 is a third-generation EGFR inhibitor, being used for the treatment of non-small cell lung cancer, overcoming the drug resistance generated from the EGFR T790M mutations, and has excellent efficacy and tolerability on NSCLC with T790M + EGFR mutations. Its major market competitor, the third-generation EGFR inhibitor, AZD9291 (AstraZeneca) has also gained FDA's groundbreaking drug eligibility.
CO-1686 is a novel, oral-administrated, targeted covalent (irreversible) inhibitor of the epidermal growth factor receptor (EGFR) mutations, being able to suppress key activation mutations and T790 drug-resistant mutations, leaving the wild-type EGFR signal unused. This drug was developed for the treatment of NSCLC patients carrying initially activated EGFR mutations and major resistant mutant T790M.
The above information is compiled and edited by Xiao Nan of Chemicalbook.

Biological activity

Rociletinib (CO-1686, AVL-301) is an irreversible, mutation-selective EGFR inhibitor that targets EGFRL858R/T790M and EGFRWT with a Ki of 21.5 nM and 303.3 nM, respectively. Phase 2.
Target: EGFR (L858R/T790M) EGFR (wt)
IC50: 21.5 nM (Ki) 303.3 nM (Ki)

In vitro study

CO-1686 inhibited the p-EGFR in EGFR-expressing cells with an IC50 ranging from 62 to 187 nM while inhibiting EGFR phosphorylation. In three WT EGFR-expressing cells, the IC50 is larger than 2,000 nM. CO-1686 can selectively inhibit the growth of mutant EGFR expressing NSCLC cells with a GI50 ranging from 7 to 32 nM while inducing apoptosis. The CO-1686-resistant NSCLC cell line exhibited a signal for epithelial-mesenchymal transition and increased susceptibility to AKT inhibitors.

In vivo studies

In all EGFR mutant models, as well as in transgenic mice expressing human EGFRL858R-and EGFRL858R/T790M, CO-1686 caused significant tumor growth inhibition in a dose-dependent manner.

Synthesis method

5-fluoro-2-nitroanisole was condensed with piperazine, acetylated and reduced to give 1-(3-methoxy-4-aminophenyl)-4-acetylpiperazine (4) In addition, use 2, 4-dichloro-5-trifluoro methyl pyrimidine to undergo condensation with 3-nitroaniline, reduction and amidation to obtain N-[3-(2-Chloro-5-trifluoromethyl-pyrimidin-4-amino) phenyl] acrylamide (7). 4 and 7 were condensed to give the EGFR inhibitor, the anticancer drug CO-1686 with a total yield of about 71% (based on 2, 4-dichloro-5-trifluoromethyl pyrimidine).
Reference: Synthesis of CO-1686 [J]. Chinese Pharmaceutical Industry, 2014, 45 (8): 710-713.
OF: (1) Lai Yisheng, male, professor, doctoral supervisor, engaged in anti-inflammatory and anti-tumor drugs studied. (2) Zhang Shan, female, graduate students, professional direction: medicinal chemistry.

Description

CO-1686 is an irreversible kinase inhibitor that specifically targets mutant forms of the epidermal growth factor receptor (EGFR) including T790M (Ki = 21.5 nM) with significantly reduced activity at the wild-type form of the receptor (Ki = 303.3 nM). CO-1686 has been shown to inhibit the proliferation of non-small cell lung cancer (NSCLC) cells expressing mutant EGFR with GI50 values ranging from 7-32 nM in vitro, inducing apoptosis. It also demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft and transgenic models dosed orally at 100 mg/kg/day.

Uses

CO 1686 is seen as an irreversible epidermal growth factor receptor (EFGR1) kinase inhibitor.

target

L858R/T790M mutant EGFR

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.

CO-1686 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from CO-1686 manufacturers

Career Henan Chemical Co
Product
CO-1686 1374640-70-6
Price
US $7.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
1000KG
Release date
2018-08-21
Career Henan Chemical Co
Product
CO-1686 1374640-70-6
Price
US $1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
1000KG
Release date
2018-08-15

1374640-70-6, CO-1686Related Search:

Volitinib Olmutinib XL-647 Genistein AZD 3759 AG 1478 HYDROCHLORIDE OSI-420 Anlotinib EGF816 Tucatinib Neratinib Poziotinib (HM781-36B) Dacomitinib Ibrutinib Afatinib AZD-9291 AVL-292 PLX4032

  • CO-1686
  • AVL-301
  • CNX-419
  • CO-1686 (AVL-301)
  • CO-1686/CO1686
  • N-[3-[[2-[[4-(4-Acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide
  • Clovis CO-1686
  • CO-1686(free base)
  • CO1686; CO-1686; CO 1686; AVL301; AVL 301; AVL-301; CNX419; CNX 419; CNX-419; ROCILETINIB.
  • Rociletinib(AVL-301,CNX-419,CO-1686)
  • N-(3-(2-(4-(4-acetylpiperazin-1-yl)-2-methoxyphenylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)phenyl)acrylamide
  • CO-1686, >=98%
  • N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
  • Rociletinib (CO1686,CNX419)
  • ROCILETINIB
  • Rociletinib(CO1686)
  • 2-Propenamide, N-[3-[[2-[[4-(4-acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-
  • Rociletinib (CO-1686, AVL-301)
  • Co 1686 N-[3-[[2-[[4-(4-Acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide
  • N-[3-[[2-[[4-(4-Acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide Co 1686
  • CO-1686(ROCILETINIB)
  • Pyridostadin
  • N-(3-((2-((4-(4-Acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl
  • CS-851
  • ROCILETINIB; AVL-301; CNX-419;CO 1686;CO1686
  • N-(3-((2-((4-(4-Acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)prop-2-enamide
  • CO-1686 (Rociletinib, AVL-301)
  • Pyridostadin 3TFA
  • CO-1686 USP/EP/BP
  • Rociletinib (CO-1686, AVL-301, CNX-419)
  • Rociletinib(free base)
  • Pazufloxacin Monomer
  • 1374640-70-6
  • C27H28F3N7O3
  • Inhibitors
  • API