2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. JND3229

JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R/T790M/C797S, EGFRWT and EGFRL858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma.

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

JND3229 Chemical Structure

JND3229 Chemical Structure

CAS No. : 2260886-64-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

JND3229 Related Antibodies

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R/T790M/C797S, EGFRWT and EGFRL858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma[1].

IC50 & Target

IC50: 5.8 nM (EGFRL858R/T790M/C797S), 6.8 nM (EGFRWT), 30.5 nM (EGFRL858R/T790M)[1].
In Vitro

JND3229 potently inhibits the proliferation of BaF3 cells (harboring the EGFRL858R/T790M/C797S and EGFR19D/T790M/C797Smutations), NCI-H1975 NSCLC cells (with EGFRT790M mutation) and A431 cancer cells (overexpressing EGFRWT) with IC50 values of 0.51, 0.32, 0.31 and 0.27 µM, respectively[1].
JND3229 (0.1, 0.3, 1, 3, 10 µM; 2 h) potently inhibits the phosphorylation of EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S in engineering BaF3 cells[1].

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

JND3229 Related Antibodies

Western Blot Analysis[1]

Cell Line: BaF3 cells (overexpressing EGFRL858R/T790M/C797S or EGFR19D/T790M/C797S)
Concentration: 0.1, 0.3, 1, 3, 10 µM
Incubation Time: 2 h
Result: Significantly inhibited the phosphorylation of EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S in a dose-dependent manner.
In Vivo

JND3229 (10 mg/kg; i.p.; twice daily for 10 days) exhibits an obvious suppression of tumor growth, and shows target inhibition in vivo[1].

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

Animal Model: BALB/c mice (bearing established BaF3-EGFR19D/T790M/C797S mouse xenograft tumors model)[1].
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; twice daily for 10 days.
Result: Caused an obvious suppression of tumor growth with a Tumor Growth Inhibition (TGI) value of 42.2%.
Showed well tolerance without obvious body weight loss or other obvious toxic sign in the treated animals.
Significantly decreased the level of phosphorylated EGFR (p-EGFR) tin the tumor tissues.
Molecular Weight

617.18

Formula

C33H41ClN8O2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC1=CC(NC2=NC(N([C@@H]3CC[C@@H](NC(CC)=O)CC3)C(N(C4=C(Cl)C=CC=C4)C5)=O)=C5C=N2)=CC=C1N6CCN(C)CC6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (20.25 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 1.6203 mL 8.1014 mL 16.2027 mL
5 mM 0.3241 mL 1.6203 mL 3.2405 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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: ≥ 1.25 mg/mL (2.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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)

g

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: 99.78%

COA (256 KB) HNMR (250 KB) RP-HPLC (138 KB) LCMS (382 KB)

Handling Instructions (2659 KB)
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6203 mL 8.1014 mL 16.2027 mL 40.5068 mL
5 mM 0.3241 mL 1.6203 mL 3.2405 mL 8.1014 mL
10 mM 0.1620 mL 0.8101 mL 1.6203 mL 4.0507 mL
15 mM 0.1080 mL 0.5401 mL 1.0802 mL 2.7005 mL
20 mM 0.0810 mL 0.4051 mL 0.8101 mL 2.0253 mL
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JND3229 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:

JND32292260886-64-2JND 3229JND-3229EGFREpidermal growth factor receptorErbB-1HER1NSCLCBaF3A431NCI-H1975cancerdrug resistanceInhibitorinhibitorinhibit

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