WF-47-JS03

Name: WF-47-JS03
Brand: MedChemExpress
SKU: HY-133551
Rating: 4.5 (1 reviews)

Cat. No.: HY-133551 Purity: 99.63%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

WF-47-JS03 is a potent and selective RET kinase inhibitor with IC₅₀s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration.

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

WF-47-JS03 Chemical Structure

CAS No. : 2561413-77-0

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 453	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 453	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2200	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3400	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.0017 μM Compound: 1; WF-47-JS03	Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay	[PMID: 32292564]
BaF3	IC₅₀	0.99 μM Compound: 1; WF-47-JS03	Inhibition of TEL/KDR (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay Inhibition of TEL/KDR (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay	[PMID: 32292564]
CHO	IC₅₀	1.2 μM Compound: 1; WF-47-JS03	Displacement of [3H]-dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method Displacement of [3H]-dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method	[PMID: 32292564]
LC-2-ad	IC₅₀	1.5 μM Compound: 1; WF-47-JS03	Cytotoxicity against human LC2/ad cells assessed as reduction in cell viability incubated for 6 days by CellTiter Glo assay Cytotoxicity against human LC2/ad cells assessed as reduction in cell viability incubated for 6 days by CellTiter Glo assay	[PMID: 32292564]

In Vitro

WF-47-JS03 inhibits Tel-KDR transfected Ba/F3 cells and Ba/F3 wild-type cell lines with IC₅₀s of 0.99 and 1.5 μM, respectively^[1].

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

In Vivo

WF-47-JS03 significantly inhibits tumor growth in RIE KIF5B-RET xenograft mice and is well tolerated at 1, 3, and 10 mg/kg in the 10 day study^[1].

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

Animal Model:	Female 6-8 week old Harlan Foxn1 nude mice with RIE-RET-KIF5B transgenic cell line
Dosage:	1, 3, 10 mg/kg
Administration:	Dosed orally, 1x daily for 10 days
Result:	Inhibited tumor growth in RIE KIF5B-RET xenograft mice.

Molecular Weight

514.66

Formula

C₃₀H₃₈N₆O₂

CAS No.

2561413-77-0

Appearance

Solid

Color

White to off-white

SMILES

NC(N1C(N=C2NC3CC(C)(C)N(C)C(C)(C)C3)=C(C4=CC(OC)=C(OC)C=C4)C=N1)=C2C5=CC=CC=C5

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

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (121.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9430 mL	9.7152 mL	19.4303 mL
5 mM	0.3886 mL	1.9430 mL	3.8861 mL
10 mM	0.1943 mL	0.9715 mL	1.9430 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, 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
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: ≥ 2.08 mg/mL (4.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

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: 99.63%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (259 KB) HNMR (223 KB) LCMS (110 KB)

Handling Instructions (2659 KB)

References

[1]. Casey J N Mathison , et al. Efficacy and Tolerability of Pyrazolo[1,5- a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma. ACS Med Chem Lett. 2020 Feb 12;11(4):558-565. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9430 mL	9.7152 mL	19.4303 mL	48.5758 mL
	5 mM	0.3886 mL	1.9430 mL	3.8861 mL	9.7152 mL
	10 mM	0.1943 mL	0.9715 mL	1.9430 mL	4.8576 mL
	15 mM	0.1295 mL	0.6477 mL	1.2954 mL	3.2384 mL
	20 mM	0.0972 mL	0.4858 mL	0.9715 mL	2.4288 mL
	25 mM	0.0777 mL	0.3886 mL	0.7772 mL	1.9430 mL
	30 mM	0.0648 mL	0.3238 mL	0.6477 mL	1.6192 mL
	40 mM	0.0486 mL	0.2429 mL	0.4858 mL	1.2144 mL
	50 mM	0.0389 mL	0.1943 mL	0.3886 mL	0.9715 mL
	60 mM	0.0324 mL	0.1619 mL	0.3238 mL	0.8096 mL
	80 mM	0.0243 mL	0.1214 mL	0.2429 mL	0.6072 mL
	100 mM	0.0194 mL	0.0972 mL	0.1943 mL	0.4858 mL

WF-47-JS03 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:

WF-47-JS032561413-77-0RETKIF5BBa/F3CCDC6LC-2/adlungcancerInhibitorinhibitorinhibit

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WF-47-JS03

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Complete Stock Solution Preparation Table

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