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Cat. No. Product Name Target Signaling Pathways
T2490 Osimertinib

AZD-9291,Mereletinib,奥希替尼

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Osimertinib (AZD-9291) 是一种 EGFR 三代抑制剂,抑制二代 EGFR 抑制剂产生的 T790M 耐药突变,具有不可逆性和口服活性。Osimertinib 具有抗肿瘤活性,用于治疗 EGFR 突变的非小细胞肺癌。
T3634 Osimertinib mesylate

甲磺酸奥希替尼,Mereletinib mesylate,奥希替尼甲磺酸盐,AZD-9291 mesylate

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Osimertinib mesylate (Mereletinib mesylate) 是一种不可逆的突变选择性 EGFR 抑制剂,对EGFRL858R 和EGFRL858R/T790M 的IC50值分别为 12 和 1 nM。
T17927 (S,R,S)-AHPC TFA

VH032-NH2 TFA,VHL ligand 1 TFA

Others; Ligand for E3 Ligase Others; PROTAC
(S,R,S)-AHPC TFA (VHL ligand 1 TFA) 是一种 VH032-based VHL ligand,可用于募集 von Hippel-Lindau (VHL)蛋白。它能够利用 linker 与靶蛋白配体连接,形成 PROTAC 分子。
T35900 JAK2-IN-7

JAK2-IN-7

JAK Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
JAK2-IN-7 是一种选择性 JAK2抑制剂,对 JAK2,SET-2 和 Ba/F3V617F 细胞的IC50为 3、11.7 和 41 nM。 JAK2-IN-7 的选择性是 JAK1, JAK3,FLT3 的 14 倍以上。JAK2-IN-7 刺激细胞周期停滞在 G0/G1 期,并诱导肿瘤细胞凋亡 (apoptosis),具有抗肿瘤活性。
T15480 HG6-64-1

HMSL 10017-101-1

Others Others
HG6-64-1 is a potent and selective inhibitor of B-Raf (IC50: 0.09 μM on B-raf V600E transformed Ba/F3 cells).
T83146 ALK-IN-27

ALK-IN-27(化合物1)是一种有效的ALK抑制剂,展现出抗肿瘤活性。在Ba/F3 CLIP1-LTK细胞中,ALK-IN-27的IC50为2.7 nM。
T78968 TRK-IN-23

Trk receptor Tyrosine Kinase/Adaptors
TRK-IN-23 (compound 24b) 是一款口服活性TRK抑制剂,对TRKA、TRKC、TRKAG595R、TRKAF589L和TRKAG667C 表现出高效的抑制作用,其IC50值分别为0.5 nM、9 nM、14 nM、4.4 nM和4.8 nM。此外,TRK-IN-23 能够诱导含有TRKAG595R和TRKAG667C突变的Ba/F3细胞系进行细胞凋亡(apoptosis)。
T63932 BCR-ABL-IN-4

BCR-ABL-IN-4 是 BCR-ABLL 抑制剂,表现出抗癌活性。BCR-ABL-IN-4 对癌细胞生长具有抑制作用,能够作用于 K562 细胞 (IC50: 0.67 nM) 和 BCR-ABL T315I 转染的 Ba/F3 细胞 (IC50: 16 nM)。
T67699L ALK/ROS1 inhibitor 2e HCL

(R)-1-(2-((2-methoxy-4-(piperazin-1-yl)phenyl)amino)pyridin-4-yl)-N-(4-(trifluoromethoxy)benzyl)piperidine-3-carboxamide hydrochloride(2365497-12-5 Free base)

Apoptosis Apoptosis
ALK/ROS1 inhibitor 2e HCL 具有抗凋亡、抗增殖和抗肿瘤活性。
T79420 FLT3-IN-22

FLT3-IN-22(化合物22f)是一款高效的FLT3抑制剂,具有针对FLT3和FLT3/D835Y极低的IC50值,分别为0.941 nM和0.199 nM。在MV4-11细胞和携带FLT3变异的Ba/F3细胞系中(涵盖FLT3-D835Y及FLT3-F691L),此抑制剂显示出显著的抗增殖能力。
T72289 Type II TRK inhibitor 1

Trk receptor Tyrosine Kinase/Adaptors
Type II TRK inhibitor 1 是有效抑制多种TRK融合蛋白及野生型的TRK抑制剂。对携有CD74-TRKAG667C及ETV6-TRKCG696C融合蛋白的Ba/F3细胞表现出抗增殖活性,其IC50值分别为6 nM与1.7 nM。
T63573 WF-47-JS03

WF-47-JS03 是选择性的、有效的、能够透过血脑屏障的 RET 激酶抑制剂,比对激酶插入域受体 (KDR) 的选择性高 500 多倍。WF-47-JS03 作用于转染 KIF5B-RET 的 Ba/F3 细胞 (IC50: 1.7 nM) 和转染 CCDC6-RET 的 LC-2/ad 肺癌细胞 (IC50: 5.3 nM)。
T37443 Aspochalasin D

Aspochalasin D is a co-metabolite originally isolated from A. microcysticus with aspochalasins A, B, and C, that was initially thought to be inactive. It has antibacterial activity against Gram-positive and Gram-negative bacteria at a concentration of 1 mg/ml. Aspochalasin D is more cytotoxic, via apoptosis, to Ba/F3-V12 cells in an IL-3-free medium than in an IL-3-containing medium (IC50s = 0.49 and 1.9 μg/ml, respectively).
T79706 TRK-IN-24

Trk receptor Tyrosine Kinase/Adaptors
TRK-IN-24(compound 10g)是一种针对Trk Receptor的抑制剂,它对TRKA、TRKC、TRKAG595R、TRKAG667C和TRKAF589L的抑制作用的IC50值分别达到5.21、4.51、6.77、1.42和6.13 nM。该化合物在BaF3-CD74-NTRK1G595R和BaF3-CD74-NTRK1G667C异种移植模型中显示出明显的抗肿瘤活性。此外,TRK-IN-24 能有效抑制携带SF、GK、xDFG等单点突变的Ba/F3细胞增殖,其IC50范围为1.43至47.56 nM。
T68581 AP23464

AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba/F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the lo...
T39732 BCR-ABL-IN-3

BCR-ABL-IN-3 is a highly effective and irreversibly binding inhibitor of Bcr-Abl, displaying a remarkable potency with an IC50 value of ≤100 nM for Ba/F3 Bcr-Abl T3151. This compound exhibits significant anti-cancer activity.

化合物

Osimertinib
Cat.No: T2490
Synonym: AZD-9291,Mereletinib,奥希替尼
Target: EGFR
Osimertinib mesylate
Cat.No: T3634
Synonym: 甲磺酸奥希替尼,Mereletinib mesylate,奥希替尼甲磺酸盐,AZD-9291 mesylate
Target: EGFR
(S,R,S)-AHPC TFA
Cat.No: T17927
Synonym: VH032-NH2 TFA,VHL ligand 1 TFA
Target: Others, Ligand for E3 Ligase
JAK2-IN-7
Cat.No: T35900
Synonym: JAK2-IN-7
Target: JAK
HG6-64-1
Cat.No: T15480
Synonym: HMSL 10017-101-1
Target: Others
ALK-IN-27
Cat.No: T83146
Synonym:
Target:
TRK-IN-23
Cat.No: T78968
Synonym:
Target: Trk receptor
BCR-ABL-IN-4
Cat.No: T63932
Synonym:
Target:
ALK/ROS1 inhibitor 2e HCL
Cat.No: T67699L
Synonym: (R)-1-(2-((2-methoxy-4-(piperazin-1-yl)phenyl)amino)pyridin-4-yl)-N-(4-(trifluoromethoxy)benzyl)piperidine-3-carboxamide hydrochloride(2365497-12-5 Free base)
Target: Apoptosis
FLT3-IN-22
Cat.No: T79420
Synonym:
Target:
Type II TRK inhibitor 1
Cat.No: T72289
Synonym:
Target: Trk receptor
WF-47-JS03
Cat.No: T63573
Synonym:
Target:
Aspochalasin D
Cat.No: T37443
Synonym:
Target:
TRK-IN-24
Cat.No: T79706
Synonym:
Target: Trk receptor
AP23464
Cat.No: T68581
Synonym:
Target:
BCR-ABL-IN-3
Cat.No: T39732
Synonym:
Target:
TargetMol Loading
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