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Cat. No. Product Name CAS No. Information
PC-62101

DCC-2618

1442472-39-0

DCC-2618 (Ripretinib, DCC2618) is a potent, oral inhibitor of singly and doubly mutated KIT with IC50 of WT (IC50=4 nM), V654A (8 nM), T670I (18 nM), D816H (5 nM), D816V; also inhibits PDGFRα/β, KDR and cFMS, robustly inhibits exon 17, exon 9/13, exon 9/14, and exon 9/17 KIT mutants, as well as exon 11/17 KIT mutants; inhibits wild type and mutant KIT phosphorylation in cancer cells, demonstrates the potential to treat KIT mutant-driven cancers including GIST, systemic mastocytosis, AML, or melanoma.

Gastric Cancer

Phase 3 Clinical

PC-62100

Avapritinib

1703793-34-3

Avapritinib (BLU-285) is a potent and highly selective inhibitor of mutant KIT and PDGFRα with IC50 of 0.6, 0.27 and 0.24 nM for KIT del557-558, KIT D816V and PDGFRA D842V, respectively; displays weak inhibition against WT KIT with IC50 of 73 nM, >150-fold more potent on KIT D816V than several important kinase antitargets such as VEGFR2, SRC and FLT3; inhibits other well-characterized disease-driving KIT mutants both in vitro and in vivo in preclinical models, demonstrates marked activity in patients with diseases associated with KIT and PDGFRA (GIST) activation loop mutations.

Gastric Cancer

Phase 1 Clinical

PC-35661

AZD3229

AZD3229 (AZD-3229) is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM); shows good margin to KDR-driven effects, also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).
PC-35619

BPR1J373

BPR1J373 is a potent, orally available multitargeted kinase inhibitor, potently inhibits FLT3, c-KIT, VEGFR1-3, Aurora A, PDGFRα, PDGFRβ, RET, and SRC with IC50 values of <100 nM; inhibits cell proliferation of myeloid leukemia cell lines and primary leukemia cells with constitutively activated c-KIT (KG-1, K562 cell with IC50 of 45 and 49 nM), also suppressed c-KIT in AML cell lines and primary AML cells; induces apoptosis by mitochondrial intrinsic pathway through upregulation of proapoptotic proteins Bax and Bak and caspase 8 and 9 activation in Kasumi-1 cells, induces cell-cycle arrest for c-KIT–driven leukemia cells via targeting different signals; effectively suppressed Kasumi-1 cells in xenograft mouse model, effectively suppresses c-KIT phosphorylation of D816V mutation.
PC-62597

Famitinib

945380-27-8 Famitinib (SHR1020) is a structural analogue of sunitinib, novel and potent multi-targeted RTK inhibitor, including c-Kit, VEGFR2/3, PDGFRβ, FLT-1/3 receptor and c-RET; demonstrates the higher potency in tumour growth inhibition in human tumour xenograft models compared with sunitinib.

Colon Cancer

Phase 3 Clinical

PC-62536

CHMFL-KIT-031

CHMFL-KIT-031 is a highly selective KIT kinase primary V559D mutant inhibitor with IC50/Kd of 28/266 nM, 10-20 fold selectivity over KIT wt; also displays 15-400-fold selectivity over other primary mutants such as L576P and secondary mutants including T670I, V654A as well as N822K and D816V; exhibits a selectivity S score (1) of 0.01 among 468 kinases/mutants in the KINOMEScan™ assay; inhibits the proliferation of BaF3-TEL-KIT-V559D cells with IC50 of 25 nM, shows potent inhibitory efficacy for KIT V559D mediated signaling pathways in cell and anti-tumor activity in vivo.
PC-60152

KBP-7018 hydrochloride

1613437-67-4 A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively; also potently inhibits FLT3, VEGFR2, Fyn, PDGFRα and VEGFR2; shows promising outcomes for the treatments of idiopathic pulmonary fibrosis (IPF).

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