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Raf
亜型選択性的な製品
Raf製品
- All (48)
- Raf阻害剤 (48)
- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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| S1267 | PLX4032 (Vemurafenib) | Vemurafenib (RG7204, RO5185426, PLX4032) は、無細胞アッセイで 31 nM の IC50 を持つ、B-RafV600E の新規かつ強力な阻害剤です。酵素アッセイでは野生型 B-Raf に対して B-RafV600E に 10 倍選択的であり、細胞選択性は 100 倍を超えることがあります。Vemurafenib (PLX4032, RG7204) は Autophagy を誘発します。 |
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| S7397 | Sorafenib (BAY 43-9006) | Sorafenib は、細胞を含まないアッセイで Raf-1 および B-Raf のマルチキナーゼ阻害剤であり、それぞれ 6 nM および 22 nM の IC50 を示します。Sorafenib は、VEGFR-2、VEGFR-3、PDGFR-β、Flt-3 および c-KIT をそれぞれ 90 nM、20 nM、57 nM、59 nM および 68 nM の IC50 で阻害します。Sorafenib は、抗腫瘍活性を持つ autophagy と apoptosis を誘導し、ferroptosis を活性化します。 |
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| S2807 | Dabrafenib (GSK2118436) | ダブラフェニブ (Dabrafenib (GSK2118436、GSK2118436A)) は変異型 BRAFV600E 特異的阻害剤 (無細胞アッセイで IC50 = 0.7 nM) であり、B-Raf(wt), c-Raf(wt) に対する効力は変異型に比べそれぞれ 7/9 倍低くなっています。 |
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| S1040 | Sorafenib Tosylate (BAY 43-9006) | Sorafenib tosylateは、無細胞アッセイにおいてIC50がそれぞれ6 nMおよび22 nMのRaf-1およびB-Rafのマルチキナーゼ阻害剤です。Sorafenib Tosylateは、VEGFR-2、VEGFR-3、PDGFR-β、Flt-3、およびc-KITをそれぞれ90 nM、20 nM、57 nM、59 nM、および68 nMのIC50で阻害します。Sorafenib Tosylateは、抗腫瘍活性を伴うautophagyとapoptosisを誘導し、ferroptosisを活性化します。 |
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| S1178 | Regorafenib (BAY 73-4506) | Regorafenibは VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) および Raf-1 に対するマルチターゲット阻害剤であり、cell-free assay における IC50 はそれぞれ 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM, 2.5 nM です。Regorafenib はオートファジーを誘導します。 |
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| S1152 | PLX-4720 | PLX-4720は、cell-freeアッセイにおいて13nMのIC50を示す強力で選択的なB-RafV600E阻害剤であり、c-Raf-1（Y340DおよびY341D変異）と同等の効力を持ち、野生型B-RafよりもB-RafV600Eに対して10倍の選択性を示します。 |
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| S1574 | Doramapimod (BIRB 796) | Doramapimod (BIRB 796) は、細胞を含まないアッセイでp38α/β/γ/δに対して38 nM、65 nM、200 nM、520 nMのIC50を持つpan-p38 MAPK阻害剤であり、THP-1細胞では0.1 nMのKdでp38αに結合し、JNK2と比較して330倍高い選択性を示します。c-RAF、Fyn、Lckに対しては弱い阻害作用を示し、ERK-1、SYK、IKK2に対しては有意な阻害作用を示しません。 |
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| S5069 | Dabrafenib Mesylate | Dabrafenib Mesylate (GSK2118436) is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.8 nM, 3.2 nM and 5 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively. | ||
| S7842 | LY3009120 | LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1. |
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| S5077 | Regorafenib (BAY-734506) Monohydrate | Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. | ||
| S2746 | AZ 628 | AZ628は、BRAF、BRAFV600E、c-Raf-1を対象とした新しいpan-Raf阻害剤であり、in cell-free assaysにおけるIC50値はそれぞれ105nM、34nM、29nMです。VEGFR2、DDR2、Lyn、Flt1、FMSなども阻害します。AZ628はapoptosisを誘導します。 |
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| S1104 | GDC-0879 | GDC-0879（AR-00341677）は、A375およびColo205細胞においてIC50が0.13 nMである新規の強力かつ選択的なB-Raf阻害剤であり、c-Rafに対しても活性を示します。他のタンパク質キナーゼに対する既知の阻害作用はありません。 |
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| S2220 | SB590885 | SB590885は、cell-freeアッセイにおいてKiが0.16 nMの強力なB-Raf阻害剤であり、c-Rafと比較してB-Rafに対して11倍高い選択性を示し、他のヒトキナーゼを阻害しません。 |
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| S7108 | LGX818 (Encorafenib) | Encorafenib is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM. Phase 3. |
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| S7291 | TAK-632 | TAK-632 は、B-Raf(wt) および C-Raf に対する IC50 がそれぞれ 8.3 nM および 1.4 nM の強力なパンRaf 阻害剤であり、in vitro アッセイでは、他の試験済みキナーゼに対しては阻害が少ないか、またはまったくありません。 |
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| S2872 | GW5074 | GW5074は、IC50が9 nMの強力で選択的なc-Raf阻害剤であり、JNK1/2/3、MEK1、MKK6/7、CDK1/2、c-Src、p38 MAP、VEGFR2、またはc-Fmsの活性には影響を及ぼしません。GW5074はLK誘導性アポトーシスを阻害します。 |
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| S2161 | RAF265 (CHIR-265) | RAF265 (CHIR-265) は、C-Raf/B-Raf/B-Raf V600E の強力で選択的な阻害剤であり、IC50 は 3～60 nM です。また、in vitroアッセイでは、EC50 が 30 nM で VEGFR2 リン酸化に対して強力な阻害作用を示します。RAF265 (CHIR-265) は細胞周期停止と apoptosis を誘導します。フェーズ2。 |
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| S4947 | Regorafenib Hydrochloride | Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. | ||
| S7170 | Avutometinib (Ro5126766, CH5126766) | Avutometinib(RO5126766,CH5126766,VS 6766, CKI-27, R-7304, RG-7304) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM,19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1. | ||
| S2202 | NVP-BHG712 | NVP-BHG712は、VEGFRとEphB4の阻害を区別する、ED50が25 nMの特異的なEphB4阻害剤です。また、c-Raf、c-Src、c-Ablに対してもそれぞれIC50が0.395 μM、1.266 μM、1.667 μMの活性を示します。 |
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| S7965 | PLX8394 (Plixorafenib, FORE8394) | Plixorafenib (PLX8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity. | ||
| S7964 | PLX7904 | PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. | ||
| S2720 | ZM 336372 | ZM 336372 (Zinc00581684) は、IC50が70 nMの強力かつ選択的なc-Raf阻害剤であり、B-RAFに対し10倍の選択性を示し、PKA/B/C、AMPK、p70S6などを阻害しません。 |
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| S8745 | Naporafenib (LXH254) | Naporafenib (LXH254) is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays. | ||
| S7121 | Tovorafenib (MLN2480) | Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) は、臨床試験中の経口選択的pan-Raf kinase阻害剤です。 | ||
| S8015 | Agerafenib (CEP-32496) | Agerafenib (CEP-32496)は、BRAF(V600E/WT)およびc-Rafの非常に強力な阻害剤であり、Kd値はそれぞれ14 nM/36 nMおよび39 nMです。また、Abl-1、c-Kit、Ret (c-Ret)、PDGFRβ、VEGFR2に対しても強力であり、MEK-1、MEK-2、ERK-1、ERK-2に対する親和性はごくわずかです。第1/2相。 | ||
| S7926 | Lifirafenib (BGB-283) | Lifirafenib (BGB-283, Beigene-283) potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant. | ||
| S8690 | RAF709 | RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), the only kinases with binding >80% at 1 μM. | ||
| S8853 | Belvarafenib | Belvarafenib is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively. | ||
| S8189 | BAW2881 (NVP-BAW2881) | BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations. | ||
| S6660 | B-Raf inhibitor 1 (Compound 13) dihydrochloride | B-Raf inhibitor 1 (Compound 13) is a type IIA Raf inhibitor which bind to the DFG-out conformation with ki of 1 nM,1 nM,and 0.3 nM for B-Raf(WT), B-Raf(V600E) and C-Raf, respectively. | ||
| S7743 | CCT196969 | CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. | ||
| S6680 | L-779450 | L-779450 is a highly potent low nanomolar inhibitor of B-raf with IC50 of 10 nM and Kd of 2.4 nM. | ||
| E1748 | HG6-64-1 | HG6-64-1 (HMSL 10017-101-1) is a highly potent and selective inhibitor of B-Raf with an IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells. | ||
| E1682 | Tinlorafenib | Tinlorafenib (PF-07284890, ARRY-461) is a potent, brain-penetrant inhibitor of BRAF targeting V600E/V600K mutations with IC50 values of 4.25 nM and 2.7 nM, respectively. It also effectively inhibits ERK phosphorylation and represents a new class of selective BRAF inhibitors for brain tumors. | ||
| E2505 | TBAP-001 | TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-Raf kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay. | ||
| S6905 | MCP110 | MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors. | ||
| E8290New | Flezurafenib | Flezurafenib is an oral inhibitor of pan-RAF with potential antineoplastic activity. | ||
| E1079 | GNE-9815 | GNE-9815 is a highly selective, pan-Raf inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for c-Raf and b-Raf, respectively. | ||
| S6538 | B-Raf IN 1 | B-Raf IN 1 is an inhibitor of Raf wih IC50 values of 24 nM and 25 nM for B-Raf and C-Raf respectively. It is selective over 13 other kinases, including PKCα, IKKβ, and PI3Kα. | ||
| E2651 | Raf inhibitor 1 | Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively. | ||
| S9621 | Donafenib (Sorafenib D3) | Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively. | ||
| E4681 | Claturafenib (PF-07799933) | Claturafenib (PF-07799933) is a brain-penetrant, selective, pan-mutant inhibitor of BRAF. It exhibits broad inhibition of pERK levels in HT29 cells with an IC50 value of 1.6 nM. PF-07799933 treatment displays antitumor activity against BRAFV600- and non-V600-mutant cancers preclinically and in treatment-refractory patients. | ||
| E1965 | NST-628 | NST-628 is a potent and well-tolerated single-agent inhibitor of both RAF and MEK. It acts as a pan-RAF–MEK molecular glue that blocks the phosphorylation and activation of MEK by RAF. | ||
| E4599 | BGB-3245(Brimarafenib) | BGB-3245(Brimarafenib, Brimarafenibum) is an inhibitor of Raf kinase. BGB-3245 displays potent effects against different RAF isoforms, including BRAF Class I/II/III mutations, BRAF fusions, and heterodimerization with CRAF in preclinical models. It also exhibits antineoplastic effects. | ||
| E0934 | Raf inhibitor 2 | Raf inhibitor 2 is a potent Raf kinase inhibitor with an IC50 of <1.0 μM. | ||
| S8755 | AZ304 | AZ304 is a synthetic inhibitor designed to interact with the ATP-binding site of wild type and V600E mutant BRAF with IC50 values of 79 nM and 38 nM, respectively. It also inhibits CRAF, p38 and CSF1R at sub 100 nM potencies. | ||
| E1649 | Exarafenib (KIN-2787) | Exarafenib(KIN-002787, KIN-2787, RAF/KIN_2787) is an orally-available, selective inhibitor of pan-RAF. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. KIN-2787 exhibits low nanomolar to picomolar potency against RAF1, BRAF, and ARAF with an IC50 of 0.06-3.46 nM with minimal activity towards non-RAF kinases. | ||
| S1267 | PLX4032 (Vemurafenib) | Vemurafenib (RG7204, RO5185426, PLX4032) は、無細胞アッセイで 31 nM の IC50 を持つ、B-RafV600E の新規かつ強力な阻害剤です。酵素アッセイでは野生型 B-Raf に対して B-RafV600E に 10 倍選択的であり、細胞選択性は 100 倍を超えることがあります。Vemurafenib (PLX4032, RG7204) は Autophagy を誘発します。 |
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| S7397 | Sorafenib (BAY 43-9006) | Sorafenib は、細胞を含まないアッセイで Raf-1 および B-Raf のマルチキナーゼ阻害剤であり、それぞれ 6 nM および 22 nM の IC50 を示します。Sorafenib は、VEGFR-2、VEGFR-3、PDGFR-β、Flt-3 および c-KIT をそれぞれ 90 nM、20 nM、57 nM、59 nM および 68 nM の IC50 で阻害します。Sorafenib は、抗腫瘍活性を持つ autophagy と apoptosis を誘導し、ferroptosis を活性化します。 |
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| S2807 | Dabrafenib (GSK2118436) | ダブラフェニブ (Dabrafenib (GSK2118436、GSK2118436A)) は変異型 BRAFV600E 特異的阻害剤 (無細胞アッセイで IC50 = 0.7 nM) であり、B-Raf(wt), c-Raf(wt) に対する効力は変異型に比べそれぞれ 7/9 倍低くなっています。 |
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| S1040 | Sorafenib Tosylate (BAY 43-9006) | Sorafenib tosylateは、無細胞アッセイにおいてIC50がそれぞれ6 nMおよび22 nMのRaf-1およびB-Rafのマルチキナーゼ阻害剤です。Sorafenib Tosylateは、VEGFR-2、VEGFR-3、PDGFR-β、Flt-3、およびc-KITをそれぞれ90 nM、20 nM、57 nM、59 nM、および68 nMのIC50で阻害します。Sorafenib Tosylateは、抗腫瘍活性を伴うautophagyとapoptosisを誘導し、ferroptosisを活性化します。 |
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| S1178 | Regorafenib (BAY 73-4506) | Regorafenibは VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) および Raf-1 に対するマルチターゲット阻害剤であり、cell-free assay における IC50 はそれぞれ 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM, 2.5 nM です。Regorafenib はオートファジーを誘導します。 |
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| S1152 | PLX-4720 | PLX-4720は、cell-freeアッセイにおいて13nMのIC50を示す強力で選択的なB-RafV600E阻害剤であり、c-Raf-1（Y340DおよびY341D変異）と同等の効力を持ち、野生型B-RafよりもB-RafV600Eに対して10倍の選択性を示します。 |
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| S1574 | Doramapimod (BIRB 796) | Doramapimod (BIRB 796) は、細胞を含まないアッセイでp38α/β/γ/δに対して38 nM、65 nM、200 nM、520 nMのIC50を持つpan-p38 MAPK阻害剤であり、THP-1細胞では0.1 nMのKdでp38αに結合し、JNK2と比較して330倍高い選択性を示します。c-RAF、Fyn、Lckに対しては弱い阻害作用を示し、ERK-1、SYK、IKK2に対しては有意な阻害作用を示しません。 |
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| S5069 | Dabrafenib Mesylate | Dabrafenib Mesylate (GSK2118436) is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.8 nM, 3.2 nM and 5 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively. | ||
| S7842 | LY3009120 | LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1. |
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| S5077 | Regorafenib (BAY-734506) Monohydrate | Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. | ||
| S2746 | AZ 628 | AZ628は、BRAF、BRAFV600E、c-Raf-1を対象とした新しいpan-Raf阻害剤であり、in cell-free assaysにおけるIC50値はそれぞれ105nM、34nM、29nMです。VEGFR2、DDR2、Lyn、Flt1、FMSなども阻害します。AZ628はapoptosisを誘導します。 |
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| S1104 | GDC-0879 | GDC-0879（AR-00341677）は、A375およびColo205細胞においてIC50が0.13 nMである新規の強力かつ選択的なB-Raf阻害剤であり、c-Rafに対しても活性を示します。他のタンパク質キナーゼに対する既知の阻害作用はありません。 |
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| S2220 | SB590885 | SB590885は、cell-freeアッセイにおいてKiが0.16 nMの強力なB-Raf阻害剤であり、c-Rafと比較してB-Rafに対して11倍高い選択性を示し、他のヒトキナーゼを阻害しません。 |
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| S7108 | LGX818 (Encorafenib) | Encorafenib is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM. Phase 3. |
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| S7291 | TAK-632 | TAK-632 は、B-Raf(wt) および C-Raf に対する IC50 がそれぞれ 8.3 nM および 1.4 nM の強力なパンRaf 阻害剤であり、in vitro アッセイでは、他の試験済みキナーゼに対しては阻害が少ないか、またはまったくありません。 |
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| S2872 | GW5074 | GW5074は、IC50が9 nMの強力で選択的なc-Raf阻害剤であり、JNK1/2/3、MEK1、MKK6/7、CDK1/2、c-Src、p38 MAP、VEGFR2、またはc-Fmsの活性には影響を及ぼしません。GW5074はLK誘導性アポトーシスを阻害します。 |
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| S2161 | RAF265 (CHIR-265) | RAF265 (CHIR-265) は、C-Raf/B-Raf/B-Raf V600E の強力で選択的な阻害剤であり、IC50 は 3～60 nM です。また、in vitroアッセイでは、EC50 が 30 nM で VEGFR2 リン酸化に対して強力な阻害作用を示します。RAF265 (CHIR-265) は細胞周期停止と apoptosis を誘導します。フェーズ2。 |
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| S4947 | Regorafenib Hydrochloride | Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. | ||
| S7170 | Avutometinib (Ro5126766, CH5126766) | Avutometinib(RO5126766,CH5126766,VS 6766, CKI-27, R-7304, RG-7304) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM,19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1. | ||
| S2202 | NVP-BHG712 | NVP-BHG712は、VEGFRとEphB4の阻害を区別する、ED50が25 nMの特異的なEphB4阻害剤です。また、c-Raf、c-Src、c-Ablに対してもそれぞれIC50が0.395 μM、1.266 μM、1.667 μMの活性を示します。 |
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| S7965 | PLX8394 (Plixorafenib, FORE8394) | Plixorafenib (PLX8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity. | ||
| S7964 | PLX7904 | PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. | ||
| S2720 | ZM 336372 | ZM 336372 (Zinc00581684) は、IC50が70 nMの強力かつ選択的なc-Raf阻害剤であり、B-RAFに対し10倍の選択性を示し、PKA/B/C、AMPK、p70S6などを阻害しません。 |
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| S8745 | Naporafenib (LXH254) | Naporafenib (LXH254) is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays. | ||
| S7121 | Tovorafenib (MLN2480) | Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) は、臨床試験中の経口選択的pan-Raf kinase阻害剤です。 | ||
| S8015 | Agerafenib (CEP-32496) | Agerafenib (CEP-32496)は、BRAF(V600E/WT)およびc-Rafの非常に強力な阻害剤であり、Kd値はそれぞれ14 nM/36 nMおよび39 nMです。また、Abl-1、c-Kit、Ret (c-Ret)、PDGFRβ、VEGFR2に対しても強力であり、MEK-1、MEK-2、ERK-1、ERK-2に対する親和性はごくわずかです。第1/2相。 | ||
| S7926 | Lifirafenib (BGB-283) | Lifirafenib (BGB-283, Beigene-283) potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant. | ||
| S8690 | RAF709 | RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), the only kinases with binding >80% at 1 μM. | ||
| S8853 | Belvarafenib | Belvarafenib is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively. | ||
| S8189 | BAW2881 (NVP-BAW2881) | BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations. | ||
| S6660 | B-Raf inhibitor 1 (Compound 13) dihydrochloride | B-Raf inhibitor 1 (Compound 13) is a type IIA Raf inhibitor which bind to the DFG-out conformation with ki of 1 nM,1 nM,and 0.3 nM for B-Raf(WT), B-Raf(V600E) and C-Raf, respectively. | ||
| S7743 | CCT196969 | CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. | ||
| S6680 | L-779450 | L-779450 is a highly potent low nanomolar inhibitor of B-raf with IC50 of 10 nM and Kd of 2.4 nM. | ||
| E1748 | HG6-64-1 | HG6-64-1 (HMSL 10017-101-1) is a highly potent and selective inhibitor of B-Raf with an IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells. | ||
| E1682 | Tinlorafenib | Tinlorafenib (PF-07284890, ARRY-461) is a potent, brain-penetrant inhibitor of BRAF targeting V600E/V600K mutations with IC50 values of 4.25 nM and 2.7 nM, respectively. It also effectively inhibits ERK phosphorylation and represents a new class of selective BRAF inhibitors for brain tumors. | ||
| E2505 | TBAP-001 | TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-Raf kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay. | ||
| S6905 | MCP110 | MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors. | ||
| E8290New | Flezurafenib | Flezurafenib is an oral inhibitor of pan-RAF with potential antineoplastic activity. | ||
| E1079 | GNE-9815 | GNE-9815 is a highly selective, pan-Raf inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for c-Raf and b-Raf, respectively. | ||
| S6538 | B-Raf IN 1 | B-Raf IN 1 is an inhibitor of Raf wih IC50 values of 24 nM and 25 nM for B-Raf and C-Raf respectively. It is selective over 13 other kinases, including PKCα, IKKβ, and PI3Kα. | ||
| E2651 | Raf inhibitor 1 | Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively. | ||
| S9621 | Donafenib (Sorafenib D3) | Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively. | ||
| E4681 | Claturafenib (PF-07799933) | Claturafenib (PF-07799933) is a brain-penetrant, selective, pan-mutant inhibitor of BRAF. It exhibits broad inhibition of pERK levels in HT29 cells with an IC50 value of 1.6 nM. PF-07799933 treatment displays antitumor activity against BRAFV600- and non-V600-mutant cancers preclinically and in treatment-refractory patients. | ||
| E1965 | NST-628 | NST-628 is a potent and well-tolerated single-agent inhibitor of both RAF and MEK. It acts as a pan-RAF–MEK molecular glue that blocks the phosphorylation and activation of MEK by RAF. | ||
| E4599 | BGB-3245(Brimarafenib) | BGB-3245(Brimarafenib, Brimarafenibum) is an inhibitor of Raf kinase. BGB-3245 displays potent effects against different RAF isoforms, including BRAF Class I/II/III mutations, BRAF fusions, and heterodimerization with CRAF in preclinical models. It also exhibits antineoplastic effects. | ||
| E0934 | Raf inhibitor 2 | Raf inhibitor 2 is a potent Raf kinase inhibitor with an IC50 of <1.0 μM. | ||
| S8755 | AZ304 | AZ304 is a synthetic inhibitor designed to interact with the ATP-binding site of wild type and V600E mutant BRAF with IC50 values of 79 nM and 38 nM, respectively. It also inhibits CRAF, p38 and CSF1R at sub 100 nM potencies. | ||
| E1649 | Exarafenib (KIN-2787) | Exarafenib(KIN-002787, KIN-2787, RAF/KIN_2787) is an orally-available, selective inhibitor of pan-RAF. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. KIN-2787 exhibits low nanomolar to picomolar potency against RAF1, BRAF, and ARAF with an IC50 of 0.06-3.46 nM with minimal activity towards non-RAF kinases. | ||
| E8290New | Flezurafenib | Flezurafenib is an oral inhibitor of pan-RAF with potential antineoplastic activity. |
Rafシグナル伝達経路
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間