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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 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。
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

Crizotinib Interm 7654 is an important intermediate for the synthesis of pharmaceutical compounds.
T1661L Crizotinib acetate

PF02341066,PF-2341066,PF 02341066,PF-02341066,PF2341066

Crizotinib, an orally bioavailable agent, belongs to the class of c-met/hepatocyte growth factor receptor (HGFR) tyrosine kinase inhibitors with potential antineoplastic activity.
T19510 2-Keto Crizotinib

PF-06260182

Others Others
2-Keto Crizotinib is an active lactam metabolite of crizotinib.
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).
T24652 Poloppin

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.
T70060 PF-06463922 acetate

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).

化合物

Crizotinib
Cat.No: T1661
Synonym: PF-02341066,克唑替尼
Target: c-Met/HGFR, ROS, ALK, Autophagy, ROS Kinase
(S)-crizotinib
Cat.No: T6357
Synonym: ent-crizotinib
Target: Apoptosis, DNA/RNA Synthesis, MTH1
Crizotinib hydrochloride
Cat.No: T8399
Synonym: 克里唑替尼盐酸,PF-02341066 hydrochloride
Target: c-Met/HGFR, ROS, ALK, Autophagy, ROS Kinase
Crizotinib Interm 7654
Cat.No: T31097
Synonym: Crizotinib Intermediate
Target:
Crizotinib acetate
Cat.No: T1661L
Synonym: PF02341066,PF-2341066,PF 02341066,PF-02341066,PF2341066
Target:
2-Keto Crizotinib
Cat.No: T19510
Synonym: PF-06260182
Target: Others
IR-Crizotinib
Cat.No: T82049
Synonym:
Target: NF-κB
KRCA-0008
Cat.No: T2641
Synonym: KRCA 0008,KRCA0008
Target: ACK, ALK
AZD-3463
Cat.No: T1967
Synonym: ALK/IGF1R inhibitor
Target: Apoptosis, IGF-1R, ALK, Autophagy
ALK-IN-1
Cat.No: T3059
Synonym: AP26113,Brigatinib,AP26113-analog
Target: EGFR, IGF-1R, ALK
Ensartinib hydrochloride
Cat.No: T22324
Synonym: Ensartinib dihydrochloride,X-396 dihydrochloride
Target: Others, Trk receptor, c-Met/HGFR, ALK
Taletrectinib free base
Cat.No: T38995
Synonym: AB-106freebase,Taletrectinib free base,IBI-344 free base,DS-6051b free base
Target: ROS Kinase
Taletrectinib
Cat.No: T22318
Synonym: DS-6051b,AB-106
Target: Trk receptor, ROS, ROS Kinase
X-376
Cat.No: T3550
Synonym: Ensartinib,X-396,恩沙替尼
Target: c-Met/HGFR, ALK
ALK/ROS1-IN-1
Cat.No: T10286
Synonym:
Target: Others
Poloppin
Cat.No: T24652
Synonym:
Target:
PF-06463922 acetate
Cat.No: T70060
Synonym:
Target:
TargetMol Loading
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