EGFR/HER2

Cat. No.

A11752

CAS No.

231277-92-2

Lapatinib (free base)

Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.

Cat. No.

A10141

CAS No.

439081-18-2

E/Z-Afatinib ((E/Z)-BIBW2992)

Synonyms: Tomtovok; (E/Z)-BIBW2992

BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases.

Cat. No.

A11051

CAS No.

1110813-31-4

Dacomitinib (PF299804, PF299)

Synonyms: PF-299804; PF-299

Dacomitinib (PF299804, PF299) is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4.

Cat. No.

A11416

CAS No.

183321-74-6

Erlotinib (OSI-774)

Synonyms: CP-358,774; CP-358774; OSI-774; Erlotinib free base.

Erlotinib is an epidermal growth factor receptor inhibitor (EGFR inhibitor). Erlotinib HCl was approved. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.

Cat. No.

A13681

CAS No.

1421373-65-0

Osimertinib (AZD-9291)

Synonyms: AZD 9291

Osimertinib (AZD-9291) is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors.

Cat. No.

A10638

CAS No.

698387-09-6

Neratinib (HKI-272)

Synonyms: HKI-272

Neratinib (HKI-272) is a tyrosine kinase inhibitor.

Cat. No.

A10242

CAS No.

383432-38-0

CP-724714

CP-724714 is an orally available, small molecule, potent HER-2 tyrosine kinase inhibitor that inhibits HER2 kinase (IC50 3.8 ng/ml) .

Cat. No.

A10362

CAS No.

183319-69-9

Erlotinib HCl

Synonyms: CP-358774; OSI-774; NSC 718781

Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).

Cat. No.

A10422

CAS No.

184475-35-2

Gefitinib (ZD1839)

Synonyms: ZD-1839; Iressa

Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells.

Cat. No.

A10678

CAS No.

183320-51-6

OSI-420

Synonyms: Desmethyl Erlotinib; CP-473420

OSI-420 (Desmethyl Erlotinib,CP-473420) is an orally active EGFR tyrosin kinase inhibitor, which inhibits receptor tyrosine kinases (TKs) by inhibition of the intercellular domain .

Cat. No.

A11022

CAS No.

153436-53-4

AG-1478 (Tyrphostin AG-1478)

Synonyms: Tyrphostin AG-1478

AG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM.

Cat. No.

A13044

CAS No.

1092364-38-9

Poziotinib

Synonyms: HM781-36B; NOV120101

Poziotinib is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.

Cat. No.

A10043

CAS No.

497839-62-0

AEE788

Synonyms: NVP-AEE788

AEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2.

Cat. No.

A10047

CAS No.

133550-30-8

AG-490

Synonyms: Tyrphostin AG490

AG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.

Cat. No.

A10116

CAS No.

848942-61-0

Sapitinib (AZD8931)

Synonyms: Momelotinib; AZD8931

AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling.

Cat. No.

A10211

CAS No.

267243-28-7

Canertinib (CI-1033)

Synonyms: PD-183805; CI-1033

Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM).

Cat. No.

A10706

CAS No.

257933-82-7

Pelitinib (EKB-569)

Synonyms: WAY-EKB 569; EKB-569

Pelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.

Cat. No.

A11028

CAS No.

451493-31-5

AV-412

Synonyms: MP-412

AV-412 is an EGFR/HER2 inhibitor that binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis.

Cat. No.

A11158

CAS No.

845272-21-1

Varlitinib (ARRY334543)

Synonyms: ARRY-334543

ARRY334543 is a potent, orally active small molecule inhibitor of EGFR and ErbB-2.

Cat. No.

A11558

CAS No.

215543-92-3

SU-5402

SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively).

Cat. No.

A18014

CAS No.

850140-72-6

Afatinib

Synonyms: BIBW 2992

Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

Cat. No.

A10053

CAS No.

148741-30-4

Tyrphostin AG 879

Synonyms: AG879

Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA.

Cat. No.

A10062

CAS No.

1050500-29-2

Allitinib tosylate (AST-1306 TsOH, AST-6)

Synonyms: AST-1306 TsOH; AST-6

AST-6 is a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, inhibits tumor growth both in vitro and in vivo

Cat. No.

A10210

CAS No.

481-74-3

Chrysophanic acid (Chrysophanol)

Synonyms: NSC 37132; NSC 646567; Chrysophanol

Chrysophanic acid (Chrysophanol) blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway.

Cat. No.

A10246

CAS No.

1012054-59-9

CUDC-101

CUDC-101 is a novel compound which inhibits multiple targets, which is designed to inhibit HDAC, EGFR and Her2.