(Rac)-JBJ-04-125-02

Cat. No.: HY-135805A Purity: ≥95.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor.

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

(Rac)-JBJ-04-125-02 Chemical Structure

CAS No. : 2140807-05-0

Size	Price	Stock
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 335	Ask For Quote & Lead Time
Solution
10 mM * 1 mL in DMSO	USD 335	Ask For Quote & Lead Time
Solid
1 mg	USD 133	Ask For Quote & Lead Time
5 mg	USD 280	Ask For Quote & Lead Time
10 mg	USD 450	Ask For Quote & Lead Time
25 mg	USD 880	Ask For Quote & Lead Time
50 mg	USD 1400	Ask For Quote & Lead Time
100 mg	USD 2250	Ask For Quote & Lead Time

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other Forms of (Rac)-JBJ-04-125-02:

JBJ-04-125-02 Get quote

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View All Isoforms

EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor^[1].

IC₅₀ & Target^[1]

EGFR (L858R/T790M)

0.26 nM (IC₅₀)

In Vitro

JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC₅₀ of 0.26 nM for EGFR^L858R/T790M^[1].

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

Molecular Weight

543.61

Formula

C₂₉H₂₆FN₅O₃S

CAS No.

2140807-05-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(N6CCNCC6)C=C5)C=C3)C4=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (459.89 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	1.8396 mL	9.1978 mL	18.3955 mL
5 mM	0.3679 mL	1.8396 mL	3.6791 mL
10 mM	0.1840 mL	0.9198 mL	1.8396 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. 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

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 (3.83 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 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 (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% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.83 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 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 (20.8 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.83 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: ≥95.0%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (251 KB) HNMR (212 KB) MS (83 KB)

Handling Instructions (2659 KB)

References

[1]. To C, et al. Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 2019 Jul;9(7):926-943. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8396 mL	9.1978 mL	18.3955 mL	45.9889 mL
	5 mM	0.3679 mL	1.8396 mL	3.6791 mL	9.1978 mL
	10 mM	0.1840 mL	0.9198 mL	1.8396 mL	4.5989 mL
	15 mM	0.1226 mL	0.6132 mL	1.2264 mL	3.0659 mL
	20 mM	0.0920 mL	0.4599 mL	0.9198 mL	2.2994 mL
	25 mM	0.0736 mL	0.3679 mL	0.7358 mL	1.8396 mL
	30 mM	0.0613 mL	0.3066 mL	0.6132 mL	1.5330 mL
	40 mM	0.0460 mL	0.2299 mL	0.4599 mL	1.1497 mL
	50 mM	0.0368 mL	0.1840 mL	0.3679 mL	0.9198 mL
	60 mM	0.0307 mL	0.1533 mL	0.3066 mL	0.7665 mL
	80 mM	0.0230 mL	0.1150 mL	0.2299 mL	0.5749 mL
	100 mM	0.0184 mL	0.0920 mL	0.1840 mL	0.4599 mL

(Rac)-JBJ-04-125-02 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:

(Rac)-JBJ-04-125-022140807-05-0EGFREpidermal growth factor receptorErbB-1HER1Allostericanti-proliferationT790M-mutantanti-tumorracemateInhibitorinhibitorinhibit

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