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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T13074 |
TAM-IN-2
|
TAM Receptor | Tyrosine Kinase/Adaptors |
TAM-IN-2 是一种 TAM 抑制剂,吡咯并三嗪化合物 0904。 | |||
T7425 |
RU-301
|
TAM Receptor | Tyrosine Kinase/Adaptors |
RU-301 是一种新型 pan-TAM 受体抑制剂,能够在 TAM 的 Gas6 和 Ig1 结构域之间的界面处结合发挥 pan-TAM 抑制活性,Kd=12 μM,IC50=10 μM。 | |||
T6982 |
SGI-7079
|
FLT; c-Met/HGFR; c-RET; TAM Receptor; Src | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
SGI7079 是 ATP-竞争性 Axl 抑制剂,能够显著抑制 SUM149 (IC50:0.43 μM)和 KPL-4 (IC50:0.16 μM)细胞增殖。 | |||
T17205 |
UNC2541
|
Others; FLT; TAM Receptor | Angiogenesis; Others; Tyrosine Kinase/Adaptors |
UNC2541 是 Mer 酪氨酸激酶特异性抑制剂,与 MerTK ATP 结合口袋结合的IC50值为 4.4 nM,对其选择性远高于 Axl,Tyro3 和 Flt3。它能够抑制磷酸化的 MerTK (pMerTK;EC50,510 nM)。 | |||
T2311 |
LDC1267
|
TAM Receptor | Tyrosine Kinase/Adaptors |
LDC1267 是一种特异性 TAM(Tyro3, Axl and Mer) 激酶抑制剂,能够作用于 Mer( IC50<5 nM)、Tyro3(IC50:8 nM) 和 Axl(IC50:29 nM)。 | |||
TQ0041 |
Ningetinib Tosylate
|
VEGFR; c-Met/HGFR; TAM Receptor | Angiogenesis; Tyrosine Kinase/Adaptors |
Ningetinib Tosylate 是口服具有活力的、小分子酪氨酸激酶抑制剂,能够抑制 c-Met (IC50:6.7 nM),VEGFR2 (IC50:1.9 nM) 和 Axl (IC50<1.0 nM)。 | |||
T2005 |
Dubermatinib
TP0903 |
Apoptosis; TAM Receptor | Apoptosis; Tyrosine Kinase/Adaptors |
Dubermatinib (TP0903) 是一种具有高效性和选择性的 Axl 受体酪氨酸激酶抑制剂,IC50值为27 nM。 | |||
T1968 |
UNC2250
|
TAM Receptor | Tyrosine Kinase/Adaptors |
UNC2250 是选择性的Mer 抑制剂,其IC50=1.7 nM,分别比相关的激酶 Axl 和 Tyro3 选择性高 160 倍和 60 倍。 | |||
T9123 |
DS-1205
|
TAM Receptor | Tyrosine Kinase/Adaptors |
DS-1205b free base 是有效的AXL 激酶选择性抑制剂,IC50为 1.3 nM。它对MER,MET 和TRKA 也有抑制作用,IC50分别为 63、104 和 407 nM。 它可以抑制细胞迁移和肿瘤生长。 | |||
T8327 |
ONO-7475
|
Trk receptor; TAM Receptor | Tyrosine Kinase/Adaptors |
ONO-7475 是一种选择性的、有效的、具有口服活性的Axl/Mer 抑制剂。它使 AXL 过表达的EGFR 突变型 NSCLC 细胞对 EGFR-TKIs 敏感,抑制耐药细胞的产生和耐药性的维持。它与 Osimertinib 联合使用,具有用于 EGFR 突变非小细胞肺癌的潜力。 | |||
T2629 |
UNC2881
|
TAM Receptor | Tyrosine Kinase/Adaptors |
UNC2881 是一种特异性Mer 激酶抑制剂,可抑制稳态的Mer 激酶磷酸化,其IC50=22 nM。 | |||
T6907 |
NPS-1034
NPS1034,NPS 1034 |
Apoptosis; c-Met/HGFR; TAM Receptor | Apoptosis; Tyrosine Kinase/Adaptors |
NPS-1034 是一种AXL 和MET 的双重抑制剂,其IC50值分别为 10.3 和 48 nM。 | |||
T21302 |
UNC569
UNC 569 |
TAM Receptor | Tyrosine Kinase/Adaptors |
UNC569 (UNC 569) 是一种ATP 竞争性的、可逆、具有口服活性的Mer 激酶抑制剂,其IC50=2.9 nM,Ki=4.3 nM。它还抑制Axl 和Tyro3,IC50分别为 37 nM 和 48 nM。它可用于研究急性淋巴细胞白血病和非典型畸胎瘤/横纹肌瘤。 | |||
TQ0021 |
Ningetinib
CT-053,CT053PTSA,宁格替尼 |
VEGFR; c-Met/HGFR; TAM Receptor | Angiogenesis; Tyrosine Kinase/Adaptors |
Ningetinib (CT-053) 是口服具有活力的、小分子酪氨酸激酶抑制剂,能够抑制 c-Met (IC50:6.7 nM),VEGFR2 (IC50:1.9 nM) 和 Axl (IC50<1.0 nM)。 | |||
T6269 |
Bemcentinib
R428,BGB324 |
TAM Receptor | Tyrosine Kinase/Adaptors |
Bemcentinib (R428) 是具有选择性的、高效的 Axl 抑制剂,其 IC50=14 nM。 | |||
T4426 |
CEP-40783
CEP 40783,RXDX-106 |
c-Met/HGFR; TAM Receptor | Tyrosine Kinase/Adaptors |
CEP-40783 (RXDX-106) 是一种有口服活性的,高效的,选择性的 AXL (IC50:7 nM) 和 c-Met (IC50:12 nM) 抑制剂。 | |||
T2699 |
BMS 777607
BMS777607,BMS-777607,BMS 817378 |
c-Met/HGFR; TAM Receptor | Tyrosine Kinase/Adaptors |
BMS 777607 (BMS 817378) 是 Met-related 抑制剂,能够抑制 c-Met (IC50:3.9 nM),Axl (IC50:1.1 nM),Ron (IC50:1.8 nM) 和 Tyro3 (IC50:4.3 nM) 的活性。 | |||
T7379 |
2-D08
|
E1/E2/E3 Enzyme; TAM Receptor | Tyrosine Kinase/Adaptors; Ubiquitination |
2-D08是小泛素样修饰蛋白抑制剂。2-D08也能抑制 Axl,IC50=0.49 nM。 | |||
T9052 |
XL092
CL-092,JUN04542 |
VEGFR; c-Met/HGFR; TAM Receptor | Angiogenesis; Tyrosine Kinase/Adaptors |
XL092 (JUN04542) 是一种ATP 竞争性的、口服有效的多受体酪氨酸激酶 (RTKs) 抑制剂,在细胞分析中的MET (IC50:15 nM)、VEGFR2 (IC50:1.6 nM)、AXL (IC50:3.4 nM) 和 MER (IC50:7.2 nM)。它具有抗肿瘤作用,具有用于研究激酶依赖性疾病的潜力。 | |||
T4409 |
Gilteritinib
吉列替尼,ASP2215 |
FLT; TAM Receptor; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Gilteritinib (ASP2215) 是一种 FLT3 抑制剂 (IC50=0.29 nM),也是一种 AXL 抑制剂 (IC50=0.73 nM),具有 ATP 竞争性、选择性和口服活性。Gilteritinib 具有抗肿瘤活性,可以用于治疗 FLT3 突变阳性的 AML。 | |||
T2586 |
Cabozantinib
卡博替尼,XL184,BMS-907351 |
Apoptosis; VEGFR; FLT; c-Met/HGFR; c-RET; TAM Receptor; c-Kit | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
Cabozantinib (XL184) 是一种多靶点酪氨酸激酶受体抑制剂,可以抑制 VEGFR2、c-Met、Kit、Axl 和 Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM)。Cabozantinib 具有抗肿瘤和抗血管生成活性。 | |||
T5164 |
Cabozantinib hydrochloride
XL184,Cabozantinib hydrochloride (849217-68-1(free base)),BMS-907351,盐酸卡博替尼 |
VEGFR; FLT; c-Met/HGFR; TAM Receptor; c-Kit; ROR | Angiogenesis; Metabolism; Tyrosine Kinase/Adaptors |
Cabozantinib hydrochloride (XL184) 是一种有效的泛酪氨酸激酶抑制剂,可抑制 VEGFR2、c-Met、Kit、Axl 和 Flt4(IC50:0.035、1.3、4.6、7 和 6 nM)。 | |||
T16806 |
RU-302
[2-[(3,5-dimethyl-1,2-oxazol-4-yl)methylsulfanyl]phenyl]-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]methanone |
TAM Receptor | Tyrosine Kinase/Adaptors |
RU-302 是一种 TAM 受体泛抑制剂,可阻断 TAM Ig1 胞外域和 Gas6 Lg 域之间的界面。 RU-302 有效阻断 Gas6 诱导的 AXL 的激活并抑制肺癌肿瘤的生长。 | |||
T6827L |
Endoxifen hydrochloride
|
Others | Others |
Endoxifen hydrochloride,Tamoxifen的主要活性代谢产物,具备较高的对雌激素受体(estrogen receptor)的亲和力和特异性,并能抑制芳香酶活性。它在乳腺癌研究中表现出潜在应用价值。 | |||
T76776 |
Emactuzumab
RO 5509554,RG 7155 |
c-Fms; TAM Receptor | Tyrosine Kinase/Adaptors |
Emactuzumab(RG 7155) 是一种针对集落刺激因子-1 受体的单克隆抗体,靶向肿瘤相关巨噬细胞 (TAM)。Emactuzumab 具有抗肿瘤活性,可抑制集落刺激因子 1 受体 (CSF1R) 的激活。Emactuzumab 对 CSF-1R 具有高亲和力,Ki 值为 0.2 nM。Emactuzumab 可阻断 CSF-1R 二聚化,可用于研究如弥漫型腱鞘巨细胞瘤(dt-GCT)类的癌症。 | |||
T77085 |
Mipasetamab
|
ADC Antibody | Antibody-drug Conjugate/ADC Related |
Mipasetamab 是一种靶向AXL 的 IgG1κ 抗体,AXL 是一种酪氨酸激酶受体,或者是 TAM 受体 (TAM Receptor)。 Mipasetamab 参与 ADCT-601 (Mipasetamab uzoptirine) 的合成,这是一种 AXL 靶向的抗体-活性分子偶联物 (ADC)。ADCT-601 具有抗肿瘤作用。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-04396 |
C-ABL/ABL1 Protein, Human, Recombinant (GST)
v-abl,ABL,JTK7,ABL proto-oncogene 1, non-receptor t... |
Human | Baculovirus Insect Cells |
c-Abl belongs to the class of tyrosine kinases and is the prototype of a subfamily which includes two members, c-Abl and Arg (Abl-related gene). Both proteins are localized at the cell membrane, actin cytoskeleton and cytosol, and c-Abl is present in the nucleus as well. c-Abl is a non-receptor tyrosine kinase that participates in multiple signaling pathways linking the cell surface, cytoskeleton, and the nucleus. Recent in vitro studies have also linked c-Abl to amyloid-beta-induced toxicity an... | |||
TMPK-00407 |
AXL Protein, Human, Recombinant (His & Avi)
AXL oncogene,Axl,EC 2.7.10.1,Tyro7,UFO,ARK,EC 2.7.10,AI32364... |
Human | HEK293 Cells |
Axl, a member of the TAM (Tyro3, Axl, Mer) family, and its inhibitors can specifically break the kinase signaling nodes, allowing advanced patients to regain drug sensitivity with improved therapeutic efficacy. Overexpression and activation of Axl receptor tyrosine kinase have been widely accepted to promote cell proliferation, chemotherapy resistance, invasion, and metastasis in several human cancers, such as lung, breast, and pancreatic cancers. AXL Protein, Human, Recombinant (His & Avi) is e... | |||
TMPK-00472 |
AXL Protein, Cynomolgus, Recombinant (His)
Tyro7,JTK11,AI323647,AXL oncogene,EC 2.7.10.1,EC 2.7.10,UFO,... |
Cynomolgus | HEK293 Cells |
Axl, a member of the TAM (Tyro3, Axl, Mer) family, and its inhibitors can specifically break the kinase signaling nodes, allowing advanced patients to regain drug sensitivity with improved therapeutic efficacy. Overexpression and activation of Axl receptor tyrosine kinase have been widely accepted to promote cell proliferation, chemotherapy resistance, invasion, and metastasis in several human cancers, such as lung, breast, and pancreatic cancers. AXL Protein, Cynomolgus, Recombinant (His) is ex... | |||
TMPK-00410 |
AXL Protein (Primary Amine Labeling), Human, Recombinant (hFc), Biotinylated
ARK,EC 2.7.10.1,EC 2.7.10,Axl,JTK11,AXL oncogene,UFO,AI32364... |
Human | HEK293 Cells |
Axl, a member of the TAM (Tyro3, Axl, Mer) family, and its inhibitors can specifically break the kinase signaling nodes, allowing advanced patients to regain drug sensitivity with improved therapeutic efficacy. Overexpression and activation of Axl receptor tyrosine kinase have been widely accepted to promote cell proliferation, chemotherapy resistance, invasion, and metastasis in several human cancers, such as lung, breast, and pancreatic cancers. AXL Protein (Primary Amine Labeling), Human, Rec... | |||
TMPK-00408 |
AXL Protein, Human, Recombinant (His & Avi), Biotinylated
AXL oncogene,EC 2.7.10.1,AI323647,Axl,JTK11,ARK,EC 2.7.10,UF... |
Human | HEK293 Cells |
Axl, a member of the TAM (Tyro3, Axl, Mer) family, and its inhibitors can specifically break the kinase signaling nodes, allowing advanced patients to regain drug sensitivity with improved therapeutic efficacy. Overexpression and activation of Axl receptor tyrosine kinase have been widely accepted to promote cell proliferation, chemotherapy resistance, invasion, and metastasis in several human cancers, such as lung, breast, and pancreatic cancers. AXL Protein, Human, Recombinant (His & Avi), Bio... | |||
TMPJ-00365 |
GAS6 Protein, Human, Recombinant (Avi & His), Biotinylated
AXLLG,Growth arrest-specific protein 6,AXL receptor... |
Human | HEK293 Cells |
Human Growth arrest-specific protein 6 (GAS6) is ligand for tyrosine-protein kinase receptors AXL, TYRO3 and MER whose signaling is implicated in cell growth and survival, cell adhesion and cell migration. GAS6/AXL signaling plays a role in various processes such as endothelial cell survival during acidification by preventing apoptosis, optimal cytokine signaling during human natural killer cell development, hepatic regeneration, gonadotropin-releasing hormone neuron survival and migration, plat... |