18
1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1661 |
Crizotinib
PF-02341066,克唑替尼 |
c-Met/HGFR; ROS; ALK; Autophagy; ROS Kinase | Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Crizotinib (PF-02341066) 是一种小分子酪氨酸激酶抑制剂,抑制 c-MET 和 ALK 受体 (IC50=8/20 nM),具有 ATP 竞争性,也可以抑制 ROS1。Crizotinib 具有抗肿瘤活性,可以抑制肿瘤生长。 | |||
T6357 |
(S)-crizotinib
ent-crizotinib |
Apoptosis; DNA/RNA Synthesis; MTH1 | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
(S)-crizotinib (ent-crizotinib) 是一种选择性MTH1(mutT 同源物)抑制剂,IC50为 330 nM。它通过抑制 MTH1 破坏核苷酸库的稳态,诱导 DNA 单链断裂的增加,激活人结肠癌细胞的 DNA 修复,在动物模型中抑制肿瘤生长。 | |||
T8399 |
Crizotinib hydrochloride
克里唑替尼盐酸,PF-02341066 hydrochloride |
c-Met/HGFR; ROS; ALK; Autophagy; ROS Kinase | Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Crizotinib hydrochloride (PF-02341066 hydrochloride) 是一种可口服的,具有选择性的 ATP 竞争性双 ALK 和 c-Met 抑制剂。它也是 ROS 原癌基因 1 抑制剂,可抑制肿瘤生长。在细胞的实验中,它抑制 NPM-ALK 的酪氨酸磷酸化和 c-Met 的酪氨酸磷酸化。 | |||
T31097 |
Crizotinib Interm 7654
Crizotinib Intermediate |
Others | Others |
Crizotinib Interm 7654 is an important intermediate for the synthesis of pharmaceutical compounds. | |||
T19510 |
2-Keto Crizotinib
PF-06260182 |
Others | Others |
2-Keto Crizotinib is an active lactam metabolite of crizotinib. | |||
T1661L |
Crizotinib acetate
PF02341066,PF-2341066,PF 02341066,PF-02341066,PF2341066 |
Others | Others |
Crizotinib, an orally bioavailable agent, belongs to the class of c-met/hepatocyte growth factor receptor (HGFR) tyrosine kinase inhibitors with potential antineoplastic activity. | |||
T82049 |
IR-Crizotinib
|
NF-κB | NF-κB |
IR-Crizotinib是一种结合了近红外染料IR-786和Crizotinib的复合物,能穿透血脑屏障及在小鼠颅内荧光定位GBM。作为NIK抑制剂,其IC50值为3.381 μM,既能有效抑制胶质瘤细胞体外生长及侵袭,也适用于体内研究,对癌症治疗具有研究意义。 | |||
T2641 |
KRCA-0008
KRCA 0008,KRCA0008 |
ACK; ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
KRCA-0008 是高效的、选择性的 ALK/Ack1 抑制剂,对ALK 和Ack1的IC50值分别为12nM 和4nM,显示出非hERG 依赖性药物活性。 | |||
T1967 |
AZD-3463
ALK/IGF1R inhibitor |
Apoptosis; IGF-1R; ALK; Autophagy | Angiogenesis; Apoptosis; Autophagy; Tyrosine Kinase/Adaptors |
AZD-3463 (ALK/IGF1R inhibitor) 是一种具有口服活性的ALK/IGF1R 抑制剂,对 ALK 作用的Ki 值为 0.75 nM。它可诱导神经母细胞瘤细胞凋亡和自噬。 | |||
T3059 |
ALK-IN-1
AP26113,Brigatinib,AP26113-analog |
EGFR; IGF-1R; ALK | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
ALK-IN-1 (AP26113) 是一种高效的、选择性的 ALK 激酶抑制剂。 | |||
T22324 |
Ensartinib hydrochloride
Ensartinib dihydrochloride,X-396 dihydrochloride |
Others; Trk receptor; c-Met/HGFR; ALK | Angiogenesis; Others; Tyrosine Kinase/Adaptors |
Ensartinib hydrochloride (X-396 dihydrochloride) 是双重的 ALK/MET 抑制剂,IC50分别 <0.4 nM 和 0.74 nM。 | |||
T38995 |
Taletrectinib free base
AB-106freebase,Taletrectinib free base,IBI-344 free base,DS-6051b free base |
ROS Kinase | Tyrosine Kinase/Adaptors |
Taletrectinib free base (AB-106 free base) 是一种新型有效且具有选择性和口服活性的 ROS1/NTRK 抑制剂。Taletrectinib free base 对重组 ROS1、NTRK1、NTRK2 和 NTRK3 具有较强的抑制作用, IC50分别以0.207、0.622、2.28 和 0.98 nM。Taletrectinib free base还对 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变有抑制作用。 | |||
T22318 |
Taletrectinib
DS-6051b,AB-106 |
Trk receptor; ROS; ROS Kinase | Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Taletrectinib (AB-106) 是具有口服活力的、选择性的 ROS1/NTRK 抑制剂。它对重组 ROS1、NTRK1、NTRK2 和 NTRK3 有较强的抑制作用,IC50值分别为 0.207、0.622、2.28 和 0.98 nM。它还抑制 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变体。 | |||
T3550 |
X-376
Ensartinib,X-396,恩沙替尼 |
c-Met/HGFR; ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
X-376 (Ensartinib) 是一种有效的ALK 抑制剂,对许多具有crizotinib 抗性的ALK 突变型和中枢神经系统转移具有高活性。它能有效地抑制野生型ALK 和ALK 变体(F1174, C1156Y, L1196M, S1206R, T1151和G1202R 突变型),IC50小于4 nM。 | |||
T10286 |
ALK/ROS1-IN-1
|
Others | Others |
ALK/ROS1-IN-1 is a potent and selective anti-crizotinib-resistant ALK/ROS1 dual inhibitor (IC50s: 0.530 μM and 0.174 μM for ROS1 and ALK enzyme). | |||
T70060 |
PF-06463922 acetate
|
Others | Others |
PF-06463922 acetate is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC). | |||
T24652 |
Poloppin
|
Others | Others |
Poloppin is a protein-protein interactions modulator of the mitotic polo-like kinases that acts by targeting mutant KRAS. It works synergistically with Crizotinib, an inhibitor of the c-MET receptor, against mutant KRAS-expressing cancer cells. | |||
T84709 |
PRO-6E
|
Others | Others |
PRO-6E是一种基于Cereblon配体的口服活性PROTAC,能在1 μM浓度下使MKN-45细胞中MET的降解率达到81.9%。该化合物有效地在体内外抑制肿瘤生长,并能诱导细胞凋亡(apoptosis)及细胞周期阻滞(结构备注:(Blue:Cereblon配体, Black: linker;Pink: ALK/c-Met抑制剂Crizotinib)。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMIJ-0115 |
Crizotinib-d5
|
||
Crizotinib-d5 是 Crizotinib 的氘代化合物。Crizotinib 的 CAS 号为 877399-52-5。Crizotinib 是 c-MET 和 ALK 受体的 ATP 竞争性小分子酪氨酸激酶抑制剂,IC50为 8和20 nM。在细胞的实验中,它抑制 NPM-ALK 的酪氨酸磷酸化和 c-Met 的酪氨酸磷酸化。它也是ROS1抑制剂。它有肿瘤生长抑制作用。 |