Description
BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties.
Product information
CAS Number: 2664214-60-0
Molecular Weight: 542.68
Formula: C30H38N8O2
Chemical Name: (11R)-5, 11, 26-trimethyl-16-[(4-methylpiperazin-1-yl)methyl]-7-oxa-4, 5, 13, 20, 22, 27-hexaazapentacyclo[22.3.1.0, .0, .0, ]octacosa-1(28), 2(6), 3, 14(19), 15, 17, 21, 24, 26-nonaen-23-one
Smiles: CC1=CC2=CC(=N1)C1C=NN(C)C=1OCCC[C@@H](C)CN1C(NC3=CC=C(CN4CCN(C)CC4)C=C13)=NC2=O |t:41|
InChiKey: AIQBYZOTCIQTGW-HXUWFJFHSA-N
InChi: InChI=1S/C30H38N8O2/c1-20-6-5-13-40-29-24(17-31-36(29)4)26-16-23(14-21(2)32-26)28(39)34-30-33-25-8-7-22(15-27(25)38(30)18-20)19-37-11-9-35(3)10-12-37/h7-8,14-17,20H,5-6,9-13,18-19H2,1-4H3,(H,33,34,39)/t20-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (460.68 mM; Need ultrasonic)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
BI-4020 inhibits p-EGFR del19 T790M C797S with an IC50 of 0.6 nM.
In Vivo:
BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice.
References:
- Engelhardt H,et al. Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors. J Med Chem. 2019 Nov 5.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.