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Cat. No. Product Name CAS No. Information
PC-62000

Enobosarm

841205-47-8

Enobosarm (GTx-024, MK-2866, Ostarine) is a selective androgen receptor modulator (SARM) for the treatment of conditions such as muscle wasting and osteoporosis.

Breast Cancer

Phase 2 Clinical

PC-61022

CC-671

1618658-88-0

CC-671 is a potent, selective, dual TTK (Mps1)/CLK2 inhibitor with IC50 of 5/3 nM, respectively; weakly inhibits DYRK3, DYRK1A, PHKG, DYRK1B, and CLK1 with IC50 of 0.1-0.3 uM, and displays excellent kinase selectivity (7/235 kinases > 80% inhibition at 3 uM); inhibits autophosphorylation of TTK at T686 or phosphorylation of SR protein 75 with IC50 of 0.057 and 0.549 uM in Cal-51 cells; demonstrates strong single agent in vivo efficacy in multiple TNBC xenograft models without significant body weight loss.

Breast Cancer

Preclinical

PC-60397

G1T38

1628256-23-4

G1T38 (Lerociclib, G1T 38) is a novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively; shows weak inhibitory effect on CDK9/cyclin T (IC50=28 nM) and CDK5/p35 (IC50=832 nM), >1,000-fold selectivity over CDK1/2/7; decreases RB1 phosphorylation, causes G1 arrest, and inhibits cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines; demonstrates equivalent or improved tumor efficacy compared to palbociclib in an ER+ breast cancer xenograft model.

Breast Cancer

Phase 2 Clinical

PC-70084

Pyrotinib

1269662-73-8

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively; displays high selectivity in a panel of different kinases such as KDR, c-Kit, PDGFRβ, c-Src and c-Met (c-Src with an IC50 of 790 nM, and others >3,000 nM); exhibits robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.

Breast Cancer

Phase 3 Clinical

PC-70083

Pyrotinib maleate

1397922-61-0

Pyrotinib maleate (SHR-1258 maleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively; displays high selectivity in a panel of different kinases such as KDR, c-Kit, PDGFRβ, c-Src and c-Met (c-Src with an IC50 of 790 nM, and others >3,000 nM); exhibits robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.

Breast Cancer

Phase 3 Clinical

PC-45734

Elacestrant dihydrochloride

1349723-93-8

Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD); inhibits ERα expression in MCF-7 cells (IC50=0.6 nM); induces the degradation of ER, inhibits ER-mediated signaling and growth of ER+ breast cancer cell lines in vitro and in vivo, and significantly inhibits tumor growth of multiple PDX models.

Breast Cancer

Phase 2 Clinical

PC-45733

Elacestrant

722533-56-4

Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD); inhibits ERα expression in MCF-7 cells (IC50=0.6 nM); induces the degradation of ER, inhibits ER-mediated signaling and growth of ER+ breast cancer cell lines in vitro and in vivo, and significantly inhibits tumor growth of multiple PDX models.

Breast Cancer

Phase 2 Clinical

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