EGFR/HER2

Cat. No.

A15977

CAS No.

1842366-97-5

Olmutinib hydrochloride

Synonyms: HM61713 hydrochloride; BI 1482694 hydrochloride

Olmutinib hydrochloride is an orally active and irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. By covalently binding to a cysteine residue in the kinase domain, it effectively disrupts signaling pathways associated with non-small cell lung cancer (NSCLC). This compound is utilized in research to study the mechanisms of EGFR-related oncogenesis as well as potential therapeutic strategies for NSCLC treatment.

Cat. No.

A16193

CAS No.

1942114-09-1

EAI045

EAI045 ia a potent and selective EGFR inhbitor. EAI045 targets selected drug-resistant EGFR mutants but spares the wild-type receptor.

Cat. No.

A16253

CAS No.

1058156-90-3

Anlotinib

Synonyms: AL3818

Anlotinib is a EGFR inhibitor extracted from patent 2015185012 A1, compound 1,which can be used to treat non-small cell lung cancer.

Cat. No.

A16254

CAS No.

171179-06-9

PD158780

PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor.

Cat. No.

A16267

CAS No.

1356962-34-9

HG-14-10-04

HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.

Cat. No.

A16361

CAS No.

1603845-32-4

TX1-85-1

TX1-85-1 is ErbB3 inhibitor. TX2-121-1 may exert Her3-dependent pharmacology through an allosteric mechanismthereby disrupting interactions between Her3 and other proteins such as Her3 or cMet consistent with results presented here and distinct from conventional kinase inhibitors, which block catalytic function.

Cat. No.

A16413

CAS No.

937263-43-9

Tucatinib (ARRY-380, Irbinitinib)

Synonyms: ONT-380; Irbinitinib; ARRY-380

ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity.

Cat. No.

A16826

CAS No.

1557267-42-1

Avitinib (AC0010)

Synonyms: AC-0010; Abivertinib

Avitinib (AC0010) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity.

Cat. No.

A16827

CAS No.

1903008-80-9

Lazertinib (YH25448, GNS-1480)

Synonyms: YH 25448; GNS1480

Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.

Cat. No.

A17068

CAS No.

1246089-97-3

Pyrotinib Racemate

Synonyms: SHR-1258 Racemate

Pyrotinib Racemate is the racemate of Pyrotinib. Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor.

Cat. No.

A17072

CAS No.

133550-49-9

Tyrphostin AG-528

Synonyms: Tyrphostin B66

Tyrphostin AG-528, also known as Tyrphostin B66, is a EGFR protein tyrosine kinase inhibitor.

Cat. No.

A17119

CAS No.

125697-92-9

Lavendustin A

Synonyms: RG-14355; NSC 678027

Lavendustin A is a selective inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase with IC50 value of 11 nM).

Cat. No.

A17123

CAS No.

122520-85-8

(E)-AG 99

Synonyms: Tyrphostin 46; Tyrphostin AG-99; AG99

AG-99 is an epidermal growth factor receptor (EGFR) kinase inhibitor with IC50 value of 10 μM.

Cat. No.

A17142

CAS No.

133550-35-3

AG-494

Synonyms: Tyrphostin AG-494

AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 μM in HT-22 cells.

Cat. No.

A17516

CAS No.

1421373-66-1

Osimertinib mesylate

Synonyms: AZD-9291 mesylate; Mereletinib mesylate

Osimertinib mesylate is a mutant-selective inhibitor of the epidermal growth factor receptor (EGFR), acting through a covalent and irreversible mechanism. It demonstrates potent biological activity with an apparent IC50 of 12 nM against the L858R mutation and 1 nM against the L858R/T790M mutation. Osimertinib mesylate is primarily utilized in research focused on overcoming T790M-mediated resistance to existing EGFR-targeted therapies in lung cancer.

Cat. No.

A17568

CAS No.

388082-78-8

Lapatinib ditosylate monohydrate

Synonyms: GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate

Lapatinib ditosylate monohydrate is a selective inhibitor of the ErbB-2 and EGFR tyrosine kinase domains. It demonstrates potent biological activity with IC50 values of 10.2 nM against EGFR and 9.8 nM against ErbB-2. This compound is commonly utilized in cancer research to investigate mechanisms of tumor growth and resistance, particularly in breast cancer models.

Cat. No.

A18243

CAS No.

2070014-82-1

Osimertinib dimesylate

Synonyms: AZD-9291; AZD 9291 (dimesylate); Mereletinib (dimesylate)

Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.

Cat. No.

A18324

CAS No.

1952236-05-3

MTX-211

MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the treatment of KRAS mutant colorectal cancer.

Cat. No.

A18327

CAS No.

136831-49-7

RG14620

Synonyms: Tyrphostin RG14620

RG14620 is an EGFR inhibitor with an IC50 of 3 μM.

Cat. No.

A18337

CAS No.

133550-34-2

AG 555

Synonyms: Tyrphostin AG 555

AG555 is a potent epidermal growth factor receptor (EGFR) kinase inhibitor.

Cat. No.

A18562

CAS No.

2267329-76-8

TQB3804 (EGFR-IN-7)

Synonyms: EGFR-IN-7

EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.

Cat. No.

A18565

CAS No.

2050906-97-1

Mutated EGFR-IN-2

Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50 ≤ 1 nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.

Cat. No.

A18857

CAS No.

1226549-49-0

DBPR112

DBPR112 is an orally active Furanopyrimidine-Based Epidermal Growth Factor Receptor inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively.

Cat. No.

A19382

CAS No.

2088323-16-2

TAS0728

TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM.

Cat. No.

A19423

CAS No.

1269662-73-8

Pyrotinib

Synonyms: SHR-1258

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.