h1975 — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T9552	BAZ1A-IN-1		Epigenetic Reader Domain
	BAZ1A-IN-1 is a potent BAZ1A inhibitor with the KD value of 0.52 μM for the BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-survival activity against cancer cell lines with high BAZ1A expression, but weak or no activity ag...		Epigenetic Reader Domain
T9927	Panitumumab		EGFR
	Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).		EGFR
T8151	Mobocertinib	tak788	EGFR
	Mobocertinib (tak788) is a potent inhibitor of epidermal growth factor receptor (EGFR) and an antineoplastic agent		EGFR
T16996	TAS6417		Apoptosis , EGFR
	TAS6417 is an EGFR inhibitor and is an efficacious drug candidate for patients with NSCLC (IC50: ranging from 1.1-8.0 nM).		Apoptosis , EGFR
T2490	Osimertinib	AZD-9291,Mereletinib	EGFR
	Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activi...		EGFR
T3634	Osimertinib mesylate	Mereletinib mesylate,AZD-9291 mesylate	EGFR
	Osimertinib mesylate (Mereletinib mesylate) is an irreversible and mutant selective EGFR inhibitor (IC50s: 12/1 nM for EGFR(L858R) and EGFR(L858R/T790M)).		EGFR
T6823	E3330		HIF/HIF Prolyl-Hydroxylase , DNA/RNA Synthesis
	E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.		HIF/HIF Prolyl-Hydroxylase , DNA/RNA Synthesis
T21312	Afatinib	Afatinib free base,BIBW 2992	EGFR , Autophagy
	Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively).		EGFR , Autophagy
T1773	Afatinib Dimaleate	BIBW2992,Afatinib,BIBW 2992MA2,Afatinib (BIBW2992) Dimaleate	EGFR , HER , Autophagy
	Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic act...		EGFR , HER , Autophagy
T22396	PF-6274484	PF 6274484	EGFR
	PF-6274484, a high affinity, irreversible covalent inhibitor of EGFR kinase with Ki of 0.14 nM, inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells with IC50 of 5.8 nM and ...		EGFR
T60146	USP8-IN-1		DUB
	USP8-IN-1 is an inhibitor of USP8 with an IC 50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI 50 of 82.04 μM [1].		DUB
T11157L	EGFR-IN-1 hydrochloride		EGFR
	EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride exhibits potent antitumor and antiproliferative activity...		EGFR
TN2755	2-Desoxy-4-epi-pulchellin		Anti-infection
	2-Desoxy-4-epi-pulchellin has potent in vitro cytotoxicities against the K562, MCF-7, Hela, DU145, U937, H1975, SGC-7901, A549, MOLT-4, and HL60 cell lines with IC50 values ranging from 0.10 to 46.7uM, while it shows sig...		Anti-infection
T63895	EGFR-IN-62
	EGFR-IN-62 is a potent inhibitor of EGFR kinase with IC50 values of 10 nM for L858R/T790 M, 29 nM for WT and 2 42 nM for L858R/T790 M/C797S. EGFR-IN-62 blocks the cell cycle of A549 and/or H1975 cells in G1/G0 phase and ...
T63531	HDAC6/HSP90-IN-1
	HDAC6/HSP90-IN-1 is a potent and selective dual inhibitor of HDAC6 (IC50: 4.3 nM) and HSP90 (IC50: 46.8 nM).HDAC6/HSP90-IN-1 downregulates PD-L1 expression in INF-γ-treated H1975 lung cancer cells.HDAC6/HSP90-IN-1 exhibi...
T74351	PROTAC EGFR degrader 3
	PROTAC EGFR Degrader 3, a highly potent molecule, exhibits remarkable cellular activity against H1975 and HCC827 cells, maintaining high selectivity. It additionally reveals the lysosome's crucial role in the degradation...
T63693	EGFR-IN-55
	EGFR-IN-55 is a potent inhibitor of EGFR, acting on EGFRWT (IC50: 70 nM) and EGFRL858R/T790M (IC50: 3.9 nM). EGFR-IN-55 was able to block the cell cycle of NCI-H1975 cells in G0/G1 phase, exhibiting anticancer effects.
T82491	EGFR-IN-90		EGFR
	EGFR-IN-90 (compound 34), an orally active EGFR inhibitor, demonstrates potent activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and effectively inhibits the proliferation of the H1975-TM cell line carrying E...		EGFR
T71436	D561-0775
	D561-0775 is a direct AMPK agonist, showing potential anti-cancer activity via inducing apoptosis, cell cycle arrest, suppressing glycolysis and cholesterol synthesis after activation of AMPK in gefitinib-resistant H1975...
T75100	DM-CO-(CH2)5-SMe
	DM-CO-(CH2)5-SMe, derived from an antibody-drug conjugate (ADC) metabolite, serves as an anticancer agent with demonstrated cytotoxicity against H1703, H1975, COLO704, and Colo720E cells [1].