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

JBJ-09-063 hydrochloride 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 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer.

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

JBJ-09-063 hydrochloride Chemical Structure

JBJ-09-063 hydrochloride Chemical Structure

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 587 In-stock
Solution
10 mM * 1 mL in DMSO USD 587 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 800 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of JBJ-09-063 hydrochloride:

JBJ-09-063 hydrochloride Related Antibodies

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JBJ-09-063 hydrochloride 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 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride 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 hydrochloride 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

593.11

Formula

C31H30ClFN4O3S
Appearance

Solid

Color

Off-white to light yellow

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.[H]Cl
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 (168.60 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 1.6860 mL 8.4301 mL 16.8603 mL
5 mM 0.3372 mL 1.6860 mL 3.3721 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

Concentration (start)

C1

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C2

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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: 99.37%

COA (252 KB) HNMR (238 KB) LCMS (97 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 1.6860 mL 8.4301 mL 16.8603 mL 42.1507 mL
5 mM 0.3372 mL 1.6860 mL 3.3721 mL 8.4301 mL
10 mM 0.1686 mL 0.8430 mL 1.6860 mL 4.2151 mL
15 mM 0.1124 mL 0.5620 mL 1.1240 mL 2.8100 mL
20 mM 0.0843 mL 0.4215 mL 0.8430 mL 2.1075 mL
25 mM 0.0674 mL 0.3372 mL 0.6744 mL 1.6860 mL
30 mM 0.0562 mL 0.2810 mL 0.5620 mL 1.4050 mL
40 mM 0.0422 mL 0.2108 mL 0.4215 mL 1.0538 mL
50 mM 0.0337 mL 0.1686 mL 0.3372 mL 0.8430 mL
60 mM 0.0281 mL 0.1405 mL 0.2810 mL 0.7025 mL
80 mM 0.0211 mL 0.1054 mL 0.2108 mL 0.5269 mL
100 mM 0.0169 mL 0.0843 mL 0.1686 mL 0.4215 mL
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JBJ-09-063 hydrochloride 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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