Cat. No.: HY-15729

Rociletinib

(Synonyms: CO-1686; AVL-301; CNX-419)

14 Cited Publications

Customer Review

Based on 14 publication(s) in Google Scholar

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

For research use only. We do not sell to patients.

Purity: 99.67%
CAS No.: 1374640-70-6
Formula: C₂₇H₂₈F₃N₇O₃
Molecular Weight:555.55

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Rociletinib Chemical Structure

CAS No.: 1374640-70-6

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

EGFR^L858R/T790M

21.5 nM (Ki)

EGFR^T790M

303.3 nM (Ki)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	GI₅₀	547 nM Compound: CO-1686	Antiproliferative activity against wild type EGFR expressing human A431 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against wild type EGFR expressing human A431 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
A-431	IC₅₀	>4331 nM Compound: CO-1686	Inhibition of wild type EGFR phosphorylation in human A431 cells after 1 hr by Western blot analysis Inhibition of wild type EGFR phosphorylation in human A431 cells after 1 hr by Western blot analysis	[PMID: 26968253]
A-431	IC₅₀	1.29 μM Compound: 4	Antiproliferative activity against wild type human A431 cells after 48 hrs by MTT assay Antiproliferative activity against wild type human A431 cells after 48 hrs by MTT assay	[PMID: 27634676]
A-431	IC₅₀	1.545 μM Compound: 2	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay	[PMID: 28033579]
A-431	IC₅₀	1.79 μM Compound: Rociletinib	Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
A-431	IC₅₀	1.794 μM Compound: 5	Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
A-431	EC₅₀	1.66 μM Compound: Rociletinib	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A-431	IC₅₀	641 nM Compound: 5; CO-1686	Cytotoxicity against human A431 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by SRB assay Cytotoxicity against human A431 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 29906114]
A-431	IC₅₀	1.29 μM Compound: Rociletinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
A-431	IC₅₀	6.01 μM Compound: Rociletinib	Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
A549	IC₅₀	1600 nM Compound: 8; CO-1686	Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA	[PMID: 26756222]
A549	IC₅₀	6.502 μM Compound: 4	Antiproliferative activity against human A549 cells harboring K-ras mutation after 48 hrs by MTT assay Antiproliferative activity against human A549 cells harboring K-ras mutation after 48 hrs by MTT assay	[PMID: 27634676]
A549	IC₅₀	3.24 μM Compound: Rociletinib	Antiproliferative activity against human A549 cells harboring EGFR K-ras mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring EGFR K-ras mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
A549	IC₅₀	3.242 μM Compound: 5	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
A549	IC₅₀	6.5 μM Compound: Rociletinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
A549	IC₅₀	7.57 μM Compound: CO-1686	Anti-proliferative activity against human A549 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human A549 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
BaF3	GI₅₀	0.94 μM Compound: 4; C01686	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
COS-7	IC₅₀	7.39 μM Compound: Rociletinib	Cytotoxicity against African green monkey COS7 cells assessed as decrease in cell viability incubated incubated for 48 hrs by MTT assay Cytotoxicity against African green monkey COS7 cells assessed as decrease in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
HaCaT	IC₅₀	262.3 nM Compound: 6; CO-1686	Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method	[PMID: 27433829]
HCC827	GI₅₀	0.03 μM Compound: CO-1686	Growth inhibition of human HCC827 cells with exon 19 deletion and delE746-A750 incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human HCC827 cells with exon 19 deletion and delE746-A750 incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
HCC827	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR Del 19 mutant expressing human HCC827 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR Del 19 mutant expressing human HCC827 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
HCC827	IC₅₀	0.031 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells harboring EGFR del E746 to A750 mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR del E746 to A750 mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
HCC827	IC₅₀	0.031 μM Compound: 5	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
HCC827	EC₅₀	0.045 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
HCC827	IC₅₀	0.031 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
HEK293	IC₅₀	0.0072 μM Compound: Rociletinib	Cytotoxicity against HEK293 cells expressing ABCG2-482-T7 in presence of methotrexate Cytotoxicity against HEK293 cells expressing ABCG2-482-T7 in presence of methotrexate	[PMID: 35944339]
HEK293	IC₅₀	0.0119 μM Compound: Rociletinib	Cytotoxicity against HEK293 cells expressing ABCG2-482-R in presence of methotrexate Cytotoxicity against HEK293 cells expressing ABCG2-482-R in presence of methotrexate	[PMID: 35944339]
NCI-H1975	GI₅₀	0.03 μM Compound: CO-1686	Growth inhibition of human NCI-H1975 cells expressing EGFR L858R/T790M mutant incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human NCI-H1975 cells expressing EGFR L858R/T790M mutant incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
NCI-H1975	IC₅₀	16 nM Compound: 8; CO-1686	Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
NCI-H1975	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR L858R / T790M double mutant expressing human NCI-H1975 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR L858R / T790M double mutant expressing human NCI-H1975 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
NCI-H1975	IC₅₀	62 nM Compound: CO-1686	Inhibition of EGFR L858R / T790M double mutant phosphorylation in human NCI-H1975 cells after 1 hr by Western blot analysis Inhibition of EGFR L858R / T790M double mutant phosphorylation in human NCI-H1975 cells after 1 hr by Western blot analysis	[PMID: 26968253]
NCI-H1975	IC₅₀	0.137 μM Compound: 4	Antiproliferative activity against human NCI-H1975 cells harboring L858R/T790M double mutant after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring L858R/T790M double mutant after 48 hrs by MTT assay	[PMID: 27634676]
NCI-H1975	IC₅₀	0.042 μM Compound: 2	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay	[PMID: 28033579]
NCI-H1975	IC₅₀	0.137 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
NCI-H1975	IC₅₀	0.299 μM Compound: 5	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
NCI-H1975	EC₅₀	0.1 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
NCI-H1975	IC₅₀	31 nM Compound: 5; CO-1686	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay	[PMID: 29906114]
NCI-H1975	IC₅₀	0.137 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
NCI-H1975	IC₅₀	0.51 μM Compound: Rociletinib	Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
NCI-H1975	IC₅₀	23 nM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells Antiproliferative activity against human NCI-H1975 cells	[PMID: 33429247]
NCI-H1975	IC₅₀	0.13 μM Compound: CO-1686	Anti-proliferative activity against human NCI-H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human NCI-H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
NCI-H358	IC₅₀	>2000 nM Compound: CO-1686	Inhibition of wild type EGFR phosphorylation in human NCI-H358 cells after 1 hr by Western blot analysis Inhibition of wild type EGFR phosphorylation in human NCI-H358 cells after 1 hr by Western blot analysis	[PMID: 26968253]
NCI-H661	GI₅₀	1.7 μM Compound: CO-1686	Growth inhibition of human NCI-H661 cells incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human NCI-H661 cells incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
PC-9	IC₅₀	79 nM Compound: 8; CO-1686	Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
PC-9	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR Del ex19 mutant expressing human PC9 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR Del ex19 mutant expressing human PC9 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
PC-9	IC₅₀	211 nM Compound: CO-1686	Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells after 1 hr by Western blot analysis Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells after 1 hr by Western blot analysis	[PMID: 26968253]
PC-9	IC₅₀	84 nM Compound: Rociletinib	Antiproliferative activity against human PC-9 cells Antiproliferative activity against human PC-9 cells	[PMID: 33429247]
PC-9	IC₅₀	0.27 μM Compound: CO-1686	Anti-proliferative activity against human PC-9 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human PC-9 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
Sf9	IC₅₀	0.002 μM Compound: CO-1686	Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	0.002 μM Compound: CO-1686	Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	0.003 μM Compound: CO-1686	Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	21.4 nM Compound: 4	Selectivity index, ratio of IC50 for human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells to IC50 for human recombinant N-terminal GST-tagged EG Selectivity index, ratio of IC50 for human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells to IC50 for human recombinant N-terminal GST-tagged EG	[PMID: 27634676]
Sf9	IC₅₀	21.5 nM Compound: 4	Inhibition of human recombinant N-terminal GST-tagged EGFR T790M/L858R double mutant cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay Inhibition of human recombinant N-terminal GST-tagged EGFR T790M/L858R double mutant cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay	[PMID: 27634676]
Sf9	IC₅₀	460 nM Compound: 4	Inhibition of human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay Inhibition of human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay	[PMID: 27634676]
SW-620	IC₅₀	10.5 μM Compound: Rociletinib	Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]

In Vitro

Rociletinib (CO-1686) (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Rociletinib (CO-1686) (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (CO-1686) (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1374640-70-6
Appearance Solid
Molecular Weight 555.55
Formula C₂₇H₂₈F₃N₇O₃
Color White to off-white
SMILES

C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O
Synonyms

CO-1686; AVL-301; CNX-419
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

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Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Acta Pharm Sin B

Rociletinib (CO-1686) enhanced the efficacy of chemotherapeutic agents in ABCG2-overexpressing cancer cells in vitro and in viv o. [Abstract]

2020 May;10(5):799-811. PMID: 32528828

Rociletinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):799-811. [Abstract]

Rociletinib enhances the anticancer effect of topotecan in the S1-MI-80 tumor xenograft model in nude mice. (A)The changes in tumor volume over time after the S1-MI-80 cell implantation (n=6). Data shown are mean±SD of tumor volumes for each group. (B) The image of tumors size in four groups excised from the mice on the 75th day after implantation.

Rociletinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):799-811. [Abstract]

The protein level of ABCG2 on MDR cells after 0, 0.25, 0.5 and 1 µmol/L rociletinib stimulation for 48 h are measured by Western blot analysis.
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
J Med Chem

Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. [Abstract]

2017 Apr 13;60(7):2944-2962. PMID: 28282122
Mol Cancer Ther

Afatinib Is a New Therapeutic Approach in Chordoma with a Unique Ability to Target EGFR and Brachyury. [Abstract]

2018 Mar;17(3):603-613. PMID: 29237806
Drug Des Devel Ther

LC-MS/MS Estimation of Rociletinib Levels in Human Liver Microsomes: Application to Metabolic Stability Estimation. [Abstract]

2021 Sep 15:15:3915-3925. PMID: 34552321
Bioorg Chem

A pomalidomide-based gefitinib PROTAC degrader effectively inhibits lung cancer progression in EGFR-TKIs-acquired resistant models by targeting EGFR degradation and ETFA-mediated ATP generation. [Abstract]

2025 Aug 9:164:108864. PMID: 40815992
Mol Cancer Res

Membrane-Associated RING-CH 8 Functions as a Novel PD-L1 E3 Ligase to Mediate PD-L1 Degradation Induced by EGFR Inhibitors. [Abstract]

2021 Oct;19(10):1622-1634. PMID: 34183449
ChemMedChem

Potent Pyrimidine and Pyrrolopyrimidine Inhibitors of Testis-Specific Serine/Threonine Kinase 2 (TSSK2). [Abstract]

2017 Nov 22;12(22):1857-1865. PMID: 28952188
Patent

US20220177473A1.
Research Square Preprint

2021 Jul.
Patent

US20190010159A1.
Oncotarget

Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation. [Abstract]

2016 Oct 25;7(43):69760-69769. PMID: 27626175
Oncotarget

Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. [Abstract]

2015 Oct 13;6(31):31313-22. PMID: 26375053

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (225.00 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8000 mL

9.0001 mL

18.0002 mL

5 mM

0.3600 mL

1.8000 mL

3.6000 mL

10 mM

0.1800 mL

0.9000 mL

1.8000 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

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Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

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 (Rociletinib) 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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 (Rociletinib) 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 (Rociletinib (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).

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8000 mL	9.0001 mL	18.0002 mL	45.0005 mL
	5 mM	0.3600 mL	1.8000 mL	3.6000 mL	9.0001 mL
	10 mM	0.1800 mL	0.9000 mL	1.8000 mL	4.5000 mL
	15 mM	0.1200 mL	0.6000 mL	1.2000 mL	3.0000 mL
	20 mM	0.0900 mL	0.4500 mL	0.9000 mL	2.2500 mL
	25 mM	0.0720 mL	0.3600 mL	0.7200 mL	1.8000 mL
	30 mM	0.0600 mL	0.3000 mL	0.6000 mL	1.5000 mL
	40 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1250 mL
	50 mM	0.0360 mL	0.1800 mL	0.3600 mL	0.9000 mL
	60 mM	0.0300 mL	0.1500 mL	0.3000 mL	0.7500 mL
	80 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5625 mL
	100 mM	0.0180 mL	0.0900 mL	0.1800 mL	0.4500 mL

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Rociletinib

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

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Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

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Human Metabolite Library

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MCE Bioactive Compound Library

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Bioactive Compound Library

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Protein Kinase Compound Library

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Mass Spectrometry Human Metabolite Library

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Publications Citing Use of MedChemExpress (MCE) Rociletinib

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (14)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Rociletinib Related Classifications

Cat. No.: HY-15729