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

Name: Rociletinib hydrobromide
Brand: MedChemExpress
SKU: HY-15729A
Rating: 5.0 (15 reviews)

Cat. No.: HY-15729A Purity: 98.04%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Rociletinib hydrobromide (CO-1686 hydrobromide) 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.

Rociletinib hydrobromide Chemical Structure

CAS No. : 1446700-26-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 70	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 70	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Rociletinib hydrobromide:

Rociletinib In-stock

13 Publications Citing Use of MCE Rociletinib hydrobromide

RT-PCR

: Rociletinib hydrobromide 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.

: Rociletinib hydrobromide 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

EGFR^L858R/T790M

21.5 nM (Ki)

EGFR^T790M

303.3 nM (Ki)

In Vitro

Rociletinib (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 (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (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

Molecular Weight

636.46

Formula

C₂₇H₂₉BrF₃N₇O₃

CAS No.

1446700-26-0

Appearance

Solid

Color

Light yellow to yellow

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.[H]Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 59 mg/mL (92.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5712 mL	7.8560 mL	15.7119 mL
5 mM	0.3142 mL	1.5712 mL	3.1424 mL
10 mM	0.1571 mL	0.7856 mL	1.5712 mL

View the Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 (3.93 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.93 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.04%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (248 KB) LCMS (260 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]

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. 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). The LUM1686 PDX xenograft study is performed by CrownBio. Briefly, LUM1686 PDX tumor fragments, harvested from donor mice, are inoculated into BALB/c nude mice. Administration of test compounds (Rociletinib) 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5712 mL	7.8560 mL	15.7119 mL	39.2798 mL
	5 mM	0.3142 mL	1.5712 mL	3.1424 mL	7.8560 mL
	10 mM	0.1571 mL	0.7856 mL	1.5712 mL	3.9280 mL
	15 mM	0.1047 mL	0.5237 mL	1.0475 mL	2.6187 mL
	20 mM	0.0786 mL	0.3928 mL	0.7856 mL	1.9640 mL
	25 mM	0.0628 mL	0.3142 mL	0.6285 mL	1.5712 mL
	30 mM	0.0524 mL	0.2619 mL	0.5237 mL	1.3093 mL
	40 mM	0.0393 mL	0.1964 mL	0.3928 mL	0.9820 mL
	50 mM	0.0314 mL	0.1571 mL	0.3142 mL	0.7856 mL
	60 mM	0.0262 mL	0.1309 mL	0.2619 mL	0.6547 mL
	80 mM	0.0196 mL	0.0982 mL	0.1964 mL	0.4910 mL

Rociletinib hydrobromide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rociletinib1446700-26-0CO-1686AVL-301CNX-419CO1686CO 1686AVL301AVL 301CNX419CNX 419EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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

Customer Review

Other Forms of Rociletinib hydrobromide:

Rociletinib hydrobromide Related Antibodies

13 Publications Citing Use of MCE Rociletinib hydrobromide

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Rociletinib hydrobromide Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Rociletinib hydrobromide Related Classifications

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