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Cat. No. Product Name CAS No. Information
PC-63027

SB-699393

1348166-93-7

SB-699393 is a potent, selective and CNS penetrant B-Raf inhibitor with Kd of 7.2 nM; possesses enhanced CNS penetration (BB ratio=0.8:1) compared with SB-590885.

PC-45573

BGB-283

1446090-77-2

BGB-283 (Lifirafenib, BGB283) is a potent pan RAF inhibitor of BRAF V600E, wt BRAF, CRAFY340/341D and wt ARAF (IC50=5-40 nM); inhibits recombinant BRAFV600E with IC50 of 23 nM; also inhibits EGFR and EGFR T790M/L858R with IC50 of 29 nM and 495 nM respectively; potently inhibits BRAF(V600E)-activated ERK phosphorylation and cell proliferation in vitro; shows tumor growth inhibition in both cell line-derived and primary human colorectal tumor xenografts bearing BRAF(V600E) mutation.

Colon Cancer

Preclinical

PC-42780

AZ 628

878739-06-1

AZ 628(AZ-628, AZ628) is a potent and selective B-Raf inhibitor with IC50s of 2.14 uM and 0.19 uM for wt Braf and Braf V600E respectively.

PC-35635

LXH254

1800398-38-2 LXH254 (LXH-254, LXH 254) is a novel potent, ATP-competitive pan-RAF inhibitor, binds to Raf proteins and inhibits Raf-mediated signal transduction pathways, inhibits proliferation of Raf-overexpressing tumor cells; demonstrates anti-proliferative activity in cell lines that contain a variety of mutations that activate MAPK signaling, blocks mutant RAS-driven signaling and cell proliferation; demonstrates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C), exhibits efficacy in numerous MAPK-driven human cancer cell lines and in xenograft tumors representing model tumors harboring human lesions in KRAS, NRAS and BRAF oncogenes.

Lung Cancer

Phase 1 Clinical

PC-35347

Balamapimod

863029-99-6 Balamapimod (MKI-833) is an orally active, reversible Ras/Raf/MEK inhibitor developed for antineoplastic potential.
PC-35100

RRD-251

131916-62-6 RRD-251 hydrochloride is a small molecule disruptor of Rb/Raf-1 interaction, potently and selectively disrupts the Rb/Raf-1 (IC50=77 nM) but not Rb/E2F, Rb/prohibitin, Rb/cyclin E, and Rb/HDAC binding; inhibits Rb to recruit Raf-1 to proliferative promoters and inhibited E2F1-dependent transcriptional activity; inhibits anchorage-dependent and anchorage-independent growth of human cancer cells; significantly inhibits tumor growth in tumors with functional Rb in vivo.
PC-35099

RRD-251 hydrochloride

72214-67-6 RRD-251 hydrochloride is a small molecule disruptor of Rb/Raf-1 interaction, potently and selectively disrupts the Rb/Raf-1 (IC50=77 nM) but not Rb/E2F, Rb/prohibitin, Rb/cyclin E, and Rb/HDAC binding; inhibits Rb to recruit Raf-1 to proliferative promoters and inhibited E2F1-dependent transcriptional activity; inhibits anchorage-dependent and anchorage-independent growth of human cancer cells; significantly inhibits tumor growth in tumors with functional Rb in vivo.

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