JBJ-09-063 free base

JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor.

For research use only. Not for human or veterinary use.

Target EGFR

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

JBJ-09-063 structure

CAS No.: 2820336-67-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 900.00	BP-02249-25mg	In stock	Get quote
50 mg	USD 1,385.00	BP-02249-50mg	In stock	Get quote
100 mg	USD 2,085.00	BP-02249-100mg	In stock	Get quote
250 mg	USD 2,885.00	BP-02249-250mg	In stock	Get quote
500 mg	USD 3,885.00	BP-02249-500mg	In stock	Get quote
1 g	USD 4,985.00	BP-02249-1g	In stock	Get quote

Need another size or custom synthesis? Request a quote.

Description

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

Biological activity

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. JBJ-09-063 is effective in H1975 cells exogenously expressing the osimertinib-resistant mutations. JBJ-09-063 exhibits IC50s of 50 nM and 6 nM in Ba/F3 cell when use alone or combination with Cetuximab (HY-P9905). 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

Identifiers

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
InChIKey: SYTVDTWRIZNVEW-UHFFFAOYSA-N

Specifications

MW (average): 556.6500
Formula: C₃₁H₂₉FN₄O₃S
CAS No.: 2820336-67-0
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 120 mg/mL

Documents

References

[1]. To C, et al. An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nat Cancer. 2022 Apr;3(4):402-417.

Same target

Search EGFR

Same research area

Search Cancer