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Cat. No. Product Name CAS No. Information
PC-43511

Capmatinib

1029712-80-8

Capmatinib (INCB-28060, INC-280) is a highly potent, selective, ATP competitive inhibitor of c-MET kinase with IC50 of 0.13 nM, displays no activity against RONβ, EGFR and HER-3; inhibits c-MET phosphorylation (IC50=1 nM) in SNU-5 human gastric cancer cell line, is slightly more potent in H596 and H1437 lung cancer cell lines that express mutant c-MET due to an exon 14 deletion and a R988C mutation; inhibits c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models.

Lung Cancer

Phase 3 Clinical

PC-63144

AZD-4635

1321514-06-0

AZD-4635 (HTL 1071) is a potent, selective and orally available adenosine 2A receptor (A2AR) inhibitor with Ki of 1.7 nM, > 30-fold selectivity over other adenosine receptors; reverses the inhibitory effects of different concentrations of adenosine in CHO cells stably expressing human A2AR with IC50 of 0.1 nM (incubated with 0.1 uM adenosine); reverses suppression and restores IFNγ secretion in cells incubated with NECA in ex vivo CD8+ T cell assay; reduces tumor burden and enhances antitumor immunity in vivo.

Lung Cancer

Phase 2 Clinical

PC-61986

AZD 4205

2091134-68-6

AZD 4205 (AZD4205) is a potent, selective JAK1 inhibitor IC50 of 73 nM and Ki of 2.8 nM, shows high selectivity against JAK2 and JAK3 with IC50 of 13,233 nM and >30,000 nM respectively; shows potent inhibition of p-STAT3 in a cell based assay of JAK1 activity with an IC50 of 128 nM and excellent selectivity across the kinome; reduces residual disease and prolongs the benefit of Osimertinib in lung cancer patients with EGFR activating mutations both in vitro and in vivo.

Lung Cancer

Phase 2 Clinical

PC-61597

CK-101

1660963-42-7

CK-101 (RX-518) is a novel potent, mutant-selective, irreversible, orally available EGFR inhibitor, overcomes T790M-mediated resistance in NSCLC; specifically targets the mutant forms of EGFR, including T790M, while exhibiting minimal activity toward WT EGFR; selectively inhibits cell proliferation of cell lines expressing both the activating (HCC827, IC50 <15 nM) and resistance mutations (NCI-H1975, IC50 <5 nM); significantly inhibits tumor growth in EGFR-mutated NSCLC tumor xenograft models, with no activity in WT EGFR tumor xenograft model.

Lung Cancer

Phase 2 Clinical

PC-61450

Avitinib maleate

1557268-88-8

Avitinib maleate (AC-0010MA, AC0010 maleate) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M; displays 43-fold greater potency over wild-type EGFR (IC50=7.68 nM); selectively inhibits mutant EGFR phosphorylation (IC50 =7.3 nM and 2.8 nM) in NCI-H1975 and NIH/3T3_TC32T8 cells, 115- and 298-fold more sensitive than that of the inhibition of wild type EGFR in A431; overcomes T790M-induced resistance in animal models and lung cancer patients without hyperglycemia or other severe adverse effects.

Lung Cancer

Phase 2 Clinical

PC-61449

Avitinib

1557267-42-1

Avitinib (AC-0010, AC0010) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M; displays 43-fold greater potency over wild-type EGFR (IC50=7.68 nM); selectively inhibits mutant EGFR phosphorylation (IC50 =7.3 nM and 2.8 nM) in NCI-H1975 and NIH/3T3_TC32T8 cells, 115- and 298-fold more sensitive than that of the inhibition of wild type EGFR in A431; overcomes T790M-induced resistance in animal models and lung cancer patients without hyperglycemia or other severe adverse effects.

Lung Cancer

Phase 2 Clinical

PC-61389

Nedisertib

1637542-33-6

Nedisertib (M3814, MSC2490484A) is a highly potent, selective, orally bioavailable inhibitor of DNA-PK; sensitizes multiple tumor cell lines to radiation therapy in vitro and strongly enhances the antitumor activity of ionizing radiation in vivo.

Lung Cancer

Phase 2 Clinical

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