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17

抑制剂 & 化合物

1

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T63448	BRAF V600E/CRAF-IN-1
	BRAF V600E/CRAF-IN-1 是 BRAFV600E/CRAF 的有效抑制剂。BRAF V600E/CRAF-IN-1 能够作用于 HCT-116 结肠癌细胞的 G0/G1 期，使细胞周期停滞，并导致细胞凋亡。BRAF V600E/CRAF-IN-1 表现出潜力进行癌症疾病的研究。
T63882	BRAF V600E/CRAF-IN-2
	BRAF V600E/CRAF-IN-2 是 BRAFV600E/CRAF 的有效抑制剂，IC50 值分别为 0.888 和 0.229 μM。BRAF V600E/CRAF-IN-2 能够诱导 HCT-116 结肠癌细胞的细胞周期停滞在 G0/G1 期，并使细胞凋亡。BRAF V600E/CRAF-IN-2 对癌症疾病表现出研究潜力。
T9638	CCT241161	Raf	MAPK
	CCT241161 is an orally active pan-RAF inhibitor, with IC50 values of 3, 6, 10, 15, and 30 nM for LCK, CRAF, SRC, V600E-BRAF, and BRAF, respectively. It displays significant activity against BRAF and NRAS mutant melanomas, as well as demonstrating anticancer cell proliferative effects [1].
T6971	Ro 5126766 CH5126766,Avutometinib,VS-6766,RO5126766	Raf; MEK	MAPK
	Ro 5126766 (CH5126766) 是双重MEK/RAF 抑制剂，抑制BRAFV600E、CRAF、MEK 和 BRAF，IC50分别为 8.2、56、160 和 190 nM。
T5172	AZ304	c-Fms; Raf; p38 MAPK; Autophagy	Autophagy; MAPK; Tyrosine Kinase/Adaptors
	AZ304 是一种 ATP 竞争性双 BRAF 激酶抑制剂，有效抑制 BRAF (WT)、BRAF (V600E) 和野生型 CRAF，IC50值分别为79、38和68 nM。具有抗肿瘤活性。它对 p38 和 CSF1R 也有抑制作用，IC50值分别为 6 nM 和 35 nM。
TQ0048	BI-882370	Raf	MAPK
	BI-882370 是高选择性的RAF 激酶抑制剂，其结合位于 BRAF 激酶的 DFG-out 无活性构象处 (ATP 结合位点)。它抑制 SRC 家族激酶，也抑制 BRAFV600E-mutant、WT BRAF 和 CRAF 激酶，IC50值分别为 0.4、0.8 和 0.6 nM。
T1886	TAK-632	Raf; FGFR; PDGFR; Aurora Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; Tyrosine Kinase/Adaptors
	TAK632 是一种有效的pan-RAF 抑制剂，对CRAF、BRAFV600E 和BRAFWT 的IC50分别为 1.4、2.4 和 8.3 nM。
T4133	CCT196969	Raf; Src	Angiogenesis; MAPK; Tyrosine Kinase/Adaptors
	CCT196969 是泛-Raf 抑制剂，抑制B-Raf、BRafV600E 和CRAF，IC50分别为 0.1、0.04、和 0.01 μM。
T3711	RAF709	Raf	MAPK
	RAF709 是RAF 抑制剂，抑制BRAF 和CRAF，IC50分别为 0.4 和 0.5 nM，具有抗肿瘤活性。
T63365	RAF-IN-1
	RAF-IN-1 是 b/cRAF 的有效抑制剂，能够作用于 cRAF (IC50: 3.8 nM)、bRAFwt (IC50: 36 nM)，bRAFV600E (IC50: 29.4 nM)，能够抑制携带 bRAFV600E 突变的 A375 和 H358 细胞系，其 GI50分别为 3.4 和 2.9 nM。
T21602	PF-04880594
	PF-04880594 是一种有效的、选择性的 RAF 抑制剂，可抑制野生型和突变型 BRAF 和 CRAF。 PF-04880594 具有抗肿瘤活性。
T36641	RAS inhibitor Abd-7
	RAS inhibitor Abd-7 is a powerful compound (Kd=51 nM) that binds to RAS and inhibits the protein-protein interaction (PPI) between RAS and its effectors. By interacting with RAS within cells, RAS inhibitor Abd-7 hinders RAS-effector interactions and suppresses endogenous RAS-dependent signaling. Additionally, RAS inhibitor Abd-7 disrupts the PPI of different mutant KRAS proteins with PI3K, CRAF, RALGDS, as well as NRAS Q61H and HRAS G12V[1].
T68267	RO5068760
	RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1/2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen-activated protein kinase pathway activation. In vitro, RO5068760 demonstrates MEK1 kinase inhibitory activity with an IC50 of 0.025 μM in a cRaf/MEK/ERK cascade assay RO5068760 showed superior efficacy in tumors harboring B-RafV600E mutation.
T79092	TH-Z827	Ras	GPCR/G Protein; MAPK
	TH-Z827为特异性针对KRAS(G12D)突变的抑制剂，IC50值为2.4 μM。此化合物不与KRAS(WT)或KRAS(G12C)结合，并可抑制KRAS(G12D)与CRAF的相互作用，其IC50值为42 μM。
T63542	SHR902275
	SHR902275 是选择性的、有效的、口服具有活力的 RAF 抑制剂，能够靶向 RAS 突变癌症。 SHR902275 能够作用于 cRAF (IC50: 1.6 nM)、bRAFwt (IC50: 10 nM)、bRAFV600E (IC50: 5.7 nM)。SHR902275 具有细胞生长抑制效果，能够作用于 H358 细胞 (GI50: 1.5 nM)、A375 细胞 (GI50: 0.17 nM)、Calu6 细胞 (GI50: 0.4 nM) 和 SK-MEL2 细胞 (GI50: 0.32 nM)。
T28510	REDX05358 REDX 05358,REDX-05358
	REDX05358 is a highly selective and potent pan RAF inhibitor with a potential therapeutic for BRAF and RAS mutant tumors. REDX05358 has improved therapeutic potential and predicted safety profile. REDX05358 demonstrates subnanomolar binding affinity for B
T63494	Antitumor agent-60
	Antitumor agent-60 是有效的抗肿瘤药物，靶向RAS-RAF 信号通路，可与CRAF 结合 (Kd: 721.3 nM)。Antitumor agent-60 能增加癌细胞中p53和ROS 水平，使细胞核呈椭圆形和不规则形态。Antitumor agent-60 够将细胞的细胞周期阻滞在 G2/M 期，并诱导细胞凋亡 (apoptosis)。在 A549 肿瘤移植模型中，Antitumor agent-60 具有一定的抑制肿瘤生长能力。

化合物

BRAF V600E/CRAF-IN-1

Cat.No: T63448

BRAF V600E/CRAF-IN-2

Cat.No: T63882

Cat.No: T9638

Target: Raf

Cat.No: T6971

Synonym: CH5126766,Avutometinib,VS-6766,RO5126766

Target: Raf, MEK

Cat.No: T5172

Target: c-Fms, Raf, p38 MAPK, Autophagy

Cat.No: TQ0048

Target: Raf

Cat.No: T1886

Target: Raf, FGFR, PDGFR, Aurora Kinase

Cat.No: T4133

Target: Raf, Src

Cat.No: T3711

Target: Raf

Cat.No: T63365

Cat.No: T21602

RAS inhibitor Abd-7

Cat.No: T36641

Cat.No: T68267

Cat.No: T79092

Target: Ras

Cat.No: T63542

Cat.No: T28510

Synonym: REDX 05358,REDX-05358

Antitumor agent-60

Cat.No: T63494

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-05095	RAF1 Protein, Human, Recombinant (His & GST) Raf-1 proto-oncogene, serine/threonine kinase,CRAF,...	Human	Baculovirus Insect Cells
	RAF1 gene is the cellular homolog of viral raf gene (v-raf). The encoded protein is a MAP kinase kinase kinase (MAP3K), which functions downstream of the Ras family of membrane associated GTPases to which it binds directly. Once activated, the cellular RAF1 protein can phosphorylate to activate the dual specificity protein kinases MEK1 and MEK2, which in turn phosphorylate to activate the serine/threonine specific protein kinases, ERK1 and ERK2. Activated ERKs are pleiotropic effectors of cell p...

重组蛋白

RAF1 Protein, Human, Recombinant (His & GST)

Cat.No: TMPY-05095

Species: Human

Expression System: Baculovirus Insect Cells

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