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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4194 |
Raf inhibitor 2
CID-25014542,CID 25014542,CID25014542 |
Raf | MAPK |
Raf inhibitor 2 (CID 25014542) 是新型 Raf 激酶抑制剂,IC50小于 1.0 μM,可用于癌症研究。 | |||
T11898 |
LXH254
|
Raf | MAPK |
LXH254 是B/C RAF 抑制剂。 | |||
T6525 |
GW 5074
GW5074,3-(3,5-二溴-4-羟基苯亚甲基)-5-碘-1,3-二氢吲哚-2-酮,Raf1 Kinase Inhibitor I |
Apoptosis; Raf | Apoptosis; MAPK |
GW 5074 (Raf1 Kinase Inhibitor I) 是一种有效且特异性的 c-Raf 抑制剂,IC50值为 9 nM。 它对 JNK1/2/3、MEK1、MKK6/7、CDK1/2、c-Src、p38 MAP、VEGFR2 或 c-Fms 的活性没有影响。 | |||
T6296 |
RAF265
CHIR-265 |
Apoptosis; Raf; VEGFR; Autophagy | Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
RAF265 (CHIR-265) 是一种 RAF/VEGFR2抑制剂。 | |||
T9585 |
GNE-9815
3-(2-cyanopropan-2-yl)-N-[2-fluoro-4-methyl-5-(7-methyl-8-oxo-7,8-dihydropyrido[2,3-d]pyridazin-3-yl)phenyl]benzamide |
Raf | MAPK |
GNE-9815 (3-(2-cyanopropan-2-yl)-N-[2-fluoro-4-methyl-5-(7-methyl-8-oxo-7,8-dihydropyrido[2,3-d]pyridazin-3-yl)phenyl]benzamide) 是一种高激酶选择性 RAF 抑制剂,可用于通过联合治疗靶向 KRAS 突变癌症。 | |||
T40284 |
B-Raf IN 2
|
Raf | MAPK |
B-Raf IN 2, compound Ia, is a highly effective and specific inhibitor of BRAF. It exhibits significant potential for cancer research. | |||
T6949 |
PLX7904
PB04 |
Raf | MAPK |
PLX7904 (PB04) 是一种有效且选择性的悖论破坏剂 RAF 抑制剂,可抑制突变 BRAF 黑色素瘤细胞中 ERK1/2 的激活。在表达突变体 RAS 的细胞中,对 BRAFV600E 的IC50值约为 5 nM。 | |||
T10157 |
Regorafénib N-oxyde (M2)
瑞戈非尼杂质 13 |
Raf; VEGFR; c-RET; PDGFR; c-Kit; Drug Metabolite | Angiogenesis; Apoptosis; MAPK; Metabolism; Tyrosine Kinase/Adaptors |
Regorafénib N-oxyde M2 是 Regorafenib 的活性代谢物。Regorafenib 是多靶点抑制剂,包括VEGFR1/2/3,PDGFRβ,Kit,RET 和 Raf-1 , IC50分别是 13/4.2/46,22,7,1.5 和 2.5 nM。 | |||
T22436 |
Takeda-6d
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Takeda-6d 是一种新型、有效的 DFG-out RAF/血管内皮生长因子受体 2 (VEGFR2) 抑制剂,IC50 分别为 7.0 nM 和 2.2 nM。 | |||
T1792L |
Regorafenib monohydrate
|
Raf; VEGFR; c-RET; PDGFR; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Regorafenib monohydrate 是一种新型口服多激酶抑制剂,对VEGFR1/2/3、PDGFRβ、Kit、RET 和Raf-1的IC50分别为 13、4.2、46、22、7、1.5 和 2.5 nM。 | |||
T11224 |
Rineterkib
ERK-IN-1 |
ERK; Raf | MAPK |
Rineterkib (ERK-IN-1) 是口服有效的RAF 和ERK1/2的抑制剂,与 KRAS-突变型非小细胞肺癌、BRAF-突变型非小细胞肺癌、KRAS-突变型胰腺癌、KRAS -突变型结肠癌和 KRAS-突变型卵巢癌尤为相关。 | |||
T38511 |
AWL-II-38.3
|
Ephrin Receptor | Tyrosine Kinase/Adaptors |
AWL-II-38.3 is a highly effective inhibitor of EphA3, a receptor for ephrin-A. It demonstrates potent kinase inhibitory activity against EphA3 and does not show significant cellular activity against Src-family kinases or b-raf [1] [2]. | |||
T2624 |
OSI-930
OSI 930,噻尔非尼 |
Apoptosis; c-Fms; Raf; VEGFR; FLT; CSF-1R; Src; c-Kit | Angiogenesis; Apoptosis; MAPK; Tyrosine Kinase/Adaptors |
OSI-930 是 Kit,KDR 和 CSF-1R (c-Fms)的口服选择性抑制剂,IC50分别为 80 nM,9 nM 和 15 nM。它具有抗肿瘤活性,靶向肿瘤中的癌细胞增殖和血管生成。它还适度抑制 Flt-1,c-Raf 和 Lck,并且对 PDGFRα/β,Flt-3和 Abl 具有较弱的抑制活性。 | |||
T8402 |
Regorafenib Hydrochloride
瑞戈非尼盐酸盐,BAY73-4506 hydrochloride |
Raf; VEGFR; c-RET; PDGFR; Autophagy | Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Regorafenib Hydrochloride (BAY73-4506 hydrochloride) 是一种新型口服多激酶抑制剂,可抑制血管生成、基质和致癌受体酪氨酸激酶,具有强大的临床前抗肿瘤活性。它靶向作用于 VEGFR1/2/3、PDGFRβ、Kit、RET 和 Raf-1,IC50值分别为 13/4.2/46、22、7、1.5 和 2.5 nM。 | |||
T60933 |
B-Raf IN 7
|
||
B-Raf IN 7 (compound 6a) 是 B-Raf 的有效抑制剂,IC50值为 110.23 nM。B-Raf IN 7 对结肠癌细胞(HCT-116)、乳腺癌细胞 (MCF-7)、肝癌细胞 (HEPG-2)、人宫颈癌细胞 (Hela) 和人前列腺癌细胞 (PC-3) 具有抗肿瘤活性。其 IC50值分别为 7.50、9.87、10.57、11.63 和 12.83 μM。 | |||
T60727 |
B-Raf IN 8
|
||
B-Raf IN 8 (compound 7g) 是 B-Raf 的有效抑制剂 (IC50 = 70.65 nM)。B-Raf IN 8 显示出抗肿瘤活性,其对肝细胞癌 (HEPG-2)、结肠癌 (HCT-116),乳腺癌 (MCF-7) 和人前列腺癌 (PC-3) 细胞的 IC50值分别为9.78、13.78、18.52 和 29.85 μM。 | |||
T36676 |
Rineterkib hydrochloride
|
||
Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 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[1]. ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the C... | |||
T79572 |
MAPK-IN-2
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
MAPK-IN-2 (化合物3h)是一种携带抗肿瘤活性的高效MAPK抑制剂。它在多个癌细胞系中有效抑制了细胞增殖,并对MAPK途径表现出强大的抑制效果(EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, CDK4/6 IC50=95和184 nM),对突变型EGFR和B-RAF亦展现出高效力(EGFRT790M IC50=69 nM, B-RAFV600E IC50=83 nM)。 | |||
T71163 |
Pimasertib HCl
|
||
Pimasertib HCl is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. Pimasertib selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activati... | |||
T64090 |
Regorafenib mesylate
|
||
Regorafenib (BAY 73-4506) mesylate 是一种口服具有活力的多靶点受体酪氨酸激酶 (tyrosine kinase) 抑制剂,能够抑制VEGFR1/2/3 (IC50=13/4.2/46 nM),PDGFRβ (IC50: 22 nM),Kit (IC50: 7 nM),RET (IC50: 1.5 nM) 和 Raf-1 (IC50: 2.5 nM)。Regorafenib mesylate 具有强大的抗肿瘤和抗血管生成作用。 | |||
T35578 |
Phosphatidylserines (sodium salt)
Phosphatidylserines (sodium salt),L-α-Phosphatidylserine |
||
Phosphatidylserine is a naturally occurring phospholipid that comprises 2-10% of total phospholipids in mammals and is enriched in the central nervous system, particularly the retina. It is anionic and found mainly on the inner leaflet of the cell membrane. It is biosynthesized from phosphatidylcholine or phosphatidylethanolamine by phosphatidyl synthase 1 (PSS1) or PSS2, respectively, in the endoplasmic reticulum (ER) and can be reversibly converted back by the same enzymes. It can also be irre... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T16011 |
Manumycin A
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Manumycin A is an antibiotic. Manumycin A induces apoptosis and exerts antitumor activity. Manumycin A inhibits exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A acts as a selective, competitive inhibitor of | |||
T35577 |
Phosphatidylserines (bovine)
|
||
Phosphatidylserine is a naturally occurring phospholipid that comprises 2-10% of total phospholipids in mammals and is enriched in the central nervous system, particularly the retina. It is anionic and found mainly on the inner leaflet of the cell membrane. It is biosynthesized from phosphatidylcholine or phosphatidylethanolamine by phosphatidyl synthase 1 (PSS1) or PSS2, respectively, in the endoplasmic reticulum and can be reversibly converted back by the same enzymes. It can also be irreversi... |