Raf Inhibitor

Brimarafenib is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor wtih antineoplastic effect.

AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity.

I194496 is a potent cystathionine γ-lyase (CSE) inhibitor, with an IC₅₀ of 0.79 mM. I194496 can inhibit the growth of human TNBC cells via the dual targeting PI3K/Akt and Ras/Raf/ERK pathway and suppress the metastasis of human TNBC cells via down-regulating Anxa2/STAT3 and VEGF/FAK/Paxillin signaling pathways.

B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC₅₀ of 24 nM.

B-Raf IN 15 (Compound 7) is a BRAF inhibitor. B-Raf IN 15 inhibits BRAF WT and BRAF V600E with IC₅₀s of 2.0 and 0.8 μM. B-Raf IN 15 can be used for the research of cancer.

KRAS G12D-IN-30 (Compound 4) is a KRAS inhibitor. KRAS G12D-IN-30 inhibits the activation of the downstream MAPK signaling cascade (Raf1-MEK-ERK) by blocking the activity of the KRAS G12 mutant. KRAS G12D-IN-30 can be used for the research of cancer.

Raf inhibitor 2 is a potent raf kinase (IC₅₀<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research.

Sorafenib-¹³C,d₃ (Bay 43-9006-¹³C,d₃) is the ¹³C, deuterated-labeled Sorafenib (HY-10201). Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.

RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a K_D of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity.

GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits K_i values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers.

Vem-L-Cy5 (compound 3)，modified with the NIR fluorophore cyanine-5 (Cy5)，is a Vemurafenib (HY-12057)-based inhibitor of BRAF. Vem-L-Cy5 targets to BRAF^V600E，and also inhibits MEK phosphorylation. Vem-L-Cy5 has cell permeability，and inhibits cell growth of many types of cancer.

SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC₅₀s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF^wt, and bRAF^V600E, respectively. SHR902275 shows cell growth inhibition with GI₅₀s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively.

CCT241161 is an orally active pan-RAF inhibitor with IC₅₀s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity.

Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAF^V600E with a K_d of 14 nM.

Encorafenib-¹³C,d₃ is the ¹³C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).

AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC₅₀s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC₅₀, 6 nM), CSF1R (IC₅₀, 35 nM). Anti-tumor activity.

Kobe2601 is a Kobe0065 (HY-15716) analogue. Kobe2601 can be used to probe the Kobe family of compounds' mechanism of action.

Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC₅₀s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv^600E and C-RAF respectively.

Cyclorasin 9A5 TFA is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC₅₀ of 120 nM.