2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. JBJ-09-063 TFA

JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer.

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

JBJ-09-063 TFA Chemical Structure

JBJ-09-063 TFA Chemical Structure

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1 mg USD 180 In-stock
5 mg USD 450 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2550 In-stock
100 mg USD 4000 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of JBJ-09-063 TFA:

JBJ-09-063 TFA Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer[1].

IC50 & Target[1]

EGFR L858R

0.147 nM (IC50)

EGFR L858R/T790M

0.063 nM (IC50)

EGFR L858R/T790M/C797S

0.083 nM (IC50)

EGFRLT/L747S

0.396 nM (IC50)

In Vitro

JBJ-09-063 is remarkably effective at inhibiting cell growth and leads to a significant increase in apoptosis, even though H3255GR cells are resistant to gefitinib as a single agent, as they contain an EGFR T790M mutation[1].
JBJ-09-063 is effective in H1975 cells exogenously expressing the osimertinib-resistant mutations[1].
JBJ-09-063 exhibits IC50s of 50 nM and 6 nM in Ba/F3 cell when use alone or combination with Cetuximab (HY-P9905)[2].

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

JBJ-09-063 TFA Related Antibodies
In Vivo

JBJ-09-063 (3 mg/kg i.v., 20 mg/kg p.o.) exhibits favorable pharmacokinetics properties and is sufficiently stable to deliver good efficacy upon oral dosing[2].

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

Animal Model: Mice[2]
Dosage: 3 mg/kg for i.v., 20 mg/kg for p.o.
Administration: i.v. and p.o.; single dosage
Result: Pharmacokinetic Parameters of JBJ-09-063 in mice[2].
Cl (mL/min/kg), i.v. T1/2 (h) Vss (L/kg) F (%) AUC 8h (ng·h/mL)
15.7 2.3 2.5 15 2398
Molecular Weight

670.67

Formula

C33H30F4N4O5S
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(C6CCN(C)CC6)C=C5)C=C3)C4=O.O=C(O)C(F)(F)F
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 : ≥ 100 mg/mL (149.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4910 mL 7.4552 mL 14.9105 mL
5 mM 0.2982 mL 1.4910 mL 2.9821 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)

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.64%

COA (247 KB) HNMR (436 KB) LCMS (131 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 (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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4910 mL 7.4552 mL 14.9105 mL 37.2762 mL
5 mM 0.2982 mL 1.4910 mL 2.9821 mL 7.4552 mL
10 mM 0.1491 mL 0.7455 mL 1.4910 mL 3.7276 mL
15 mM 0.0994 mL 0.4970 mL 0.9940 mL 2.4851 mL
20 mM 0.0746 mL 0.3728 mL 0.7455 mL 1.8638 mL
25 mM 0.0596 mL 0.2982 mL 0.5964 mL 1.4910 mL
30 mM 0.0497 mL 0.2485 mL 0.4970 mL 1.2425 mL
40 mM 0.0373 mL 0.1864 mL 0.3728 mL 0.9319 mL
50 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7455 mL
60 mM 0.0249 mL 0.1243 mL 0.2485 mL 0.6213 mL
80 mM 0.0186 mL 0.0932 mL 0.1864 mL 0.4660 mL
100 mM 0.0149 mL 0.0746 mL 0.1491 mL 0.3728 mL
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JBJ-09-063 TFA 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:

JBJ-09-063EGFREpidermal growth factor receptorErbB-1HER1EGFR-mutantlung cancerTKI-sensitiveresistantH3255GRH1975Ba/F3AnticancerInhibitorinhibitorinhibit

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