Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T39827 | c-ABL-IN-1 | ||
C-ABL-IN-1 is a new and specific inhibitor of the c-Abl protein, which effectively prevents the progression of neurodegeneration observed in Parkinson's disease. | |||
T21785 |
AG957
|
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Tyrphostin AG957 是一种酪氨酸激酶抑制剂,具有抗BCR/ABL 酪氨酸激酶活性。它能够抑制p210bcr/abl 酶活性 (IC50:2.9 μM)。 | |||
T4320 |
Flumatinib
HHGV678 |
Bcr-Abl; PDGFR; c-Kit | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Flumatinib (HHGV678) 是一种具有口服活性的选择性 Bcr-Abl 抑制剂,能够作用于 c-Abl (IC50:1.2 nM),PDGFRβ (IC50:307.6 nM) 和 c-Kit (IC50:665.5 nM)。 | |||
T7861 |
Flumatinib mesylate
甲磺酸氟马替尼/氟马替尼,HHGV678 mesylate,甲磺酸氟马替尼 |
Bcr-Abl; PDGFR; c-Kit | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Flumatinib mesylate (HHGV678 mesylate) 是一种具有口服活性的选择性Bcr-Abl 抑制剂,能够作用于 c-Abl (IC50:1.2 nM),PDGFRβ (IC50:307.6 nM) 和 c-Kit (IC50:665.5 nM)。 | |||
T4191 |
Multi-kinase inhibitor 1
Multi-kinase inhibitor I |
Others; Bcr-Abl; PDGFR; c-Kit | Angiogenesis; Cytoskeletal Signaling; Others; Tyrosine Kinase/Adaptors |
Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) 是多激酶抑制剂。它有用于导致与酪氨酸激酶活性异常或失控有关的疾病或失调的潜力,特别是与c-Kit,PDGF-R,Bcr-abl 活性相关的疾病。 | |||
T11641 |
N-Desmethyl imatinib
Imatinib metabolite N-Desmethyl imatinib,Norimatinib,N-去甲基伊马替尼 |
Bcr-Abl; PDGFR; c-Kit; Drug Metabolite | Angiogenesis; Cytoskeletal Signaling; Metabolism; Tyrosine Kinase/Adaptors |
N-Desmethyl imatinib (Imatinib metabolite N-Desmethyl imatinib) 是 Imatinib 的代谢物。Imatinib 是一个靶向 c-Kit、v-Abl 和 PDGFR 的多靶点抑制剂。 | |||
T4053 |
AST 487
NVP-AST 487 |
VEGFR; FLT; c-RET; Bcr-Abl; c-Kit | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
AST 487 (NVP-AST 487) 是 RET 激酶抑制剂 (IC50:880 nM),能够抑制 RET 自磷酸化,及下游效应器激活,也抑制 Flt-3 (IC50:520 nM)。 | |||
T1621 |
Imatinib Mesylate
甲磺酸伊马替尼,ST-1571 Mesylate,STI-571,CGP-57148B |
Bcr-Abl; PDGFR; c-Kit; Autophagy | Angiogenesis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Imatinib Mesylate (STI-571) 是一种酪氨酸激酶受体抑制剂,具有抗肿瘤活性,对 v-Abl、c-Kit 和 PDGFR 的 IC50 分别为 0.6 μM、0.1 μM 和 0.1 μM。 | |||
T6230 |
Imatinib
伊马替尼,STI571,CGP057148B,ST-1571 |
SARS-CoV; Bcr-Abl; PDGFR; c-Kit; Autophagy | Angiogenesis; Autophagy; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors |
Imatinib (STI571) 是一种多靶点受体酪氨酸激酶抑制剂,可选择性抑制 BCR/ABL、v-Abl、PDGFR、c-kit 等激酶活性,具有口服活性。Imatinib 具有抗肿瘤活性,可用于治疗慢性粒细胞白血病。 | |||
T61546 |
c-ABL-IN-3
|
||
c-ABL-IN-3, a highly effective c-Abl inhibitor, exhibits promising potential for studying neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS) and Parkinson's disease (PD), as well as cancer [1]. The activation of c-Abl has been strongly implicated in a range of diseases, notably cancer [1]. It offers valuable opportunities for research in these fields [1]. | |||
T61128 | c-ABL-IN-2 | ||
C-ABL-IN-2 is a highly effective inhibitor of the c-Abl protein, which plays a significant role in the development of several diseases, including cancer. This compound exhibits promise for investigating neurodegenerative disorders such as amyotrophic lateral sclerosis (ALS) and Parkinson's disease (PD), as well as cancer. (Source: WO2020260871A1, compound 25) [1]. | |||
T62065 |
c-ABL-IN-4
|
||
c-ABL-IN-4 是有效的c-Abl 抑制剂。 | |||
T79716 |
c-ABL-IN-5
|
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
c-ABL-IN-5是一种选择性c-Abl抑制剂,具有神经保护功能。该化合物显示出血脑屏障渗透性、代谢稳定性和优良的药物动力学特性。经[18F]标记的c-ABL-IN-5(化合物[18F]3)可用作PET示踪剂,以评估疾病改善的功效。此外,c-ABL-IN-5适用于帕金森病(PD)等神经退行性疾病的研究。 | |||
T4618 |
BGG463
K 0859 |
Bcr-Abl; CDK | Angiogenesis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
BGG463 (K 0859) 是一种具有口服活性的 II 型 CDK2的抑制剂,可抑制 c-ABL-T334I、BCR-ABL 和 BCR-ABL-T315I 变体,IC50分别为 0.25 μM、0.09 μM 和 0.590 μM。 | |||
T6348 |
NVP-BHG712
|
Raf; Bcr-Abl; Src; Ephrin Receptor | Angiogenesis; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors |
NVP-BHG712 是一种特异性的 EphB4 抑制剂,ED50=25 nM,可区分 VEGFR 和 EphB4 抑制。它还显示对 c-Raf (IC50:0.395 μM)、c-Src (IC50:1.266 μM) 和 c-Abl (IC50:1.667 μM) 的活性。 | |||
T3935 |
1-Naphthyl PP1
4 -氨基- 1 -叔丁基- 3 -(1' -萘基)吡唑并[3,4 - D]嘧啶,1-NA-PP 1 |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
1-Naphthyl PP1 (1-NA-PP 1) 是选择性的src 家族激酶抑制剂,能够抑制 v-Src (IC50:1.0 μM)、c-Fyn (IC50:0.6 μM)、c-Abl (IC50:0.6 μM)、CDK2 (IC50:18 μM) 和 CAMK II (IC50:22 μM)。 | |||
T22552L |
AD57
|
Bcr-Abl; Src | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
AD57是c-Src 和Abl 的有效抑制剂,IC50分别为0.025μM 和0.041μM。 | |||
T15164 |
DPH
|
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
DPH 是一种有效的细胞渗透的 c-Abl 激活剂。DPH 在刺激 c-Abl 活化方面显示出强大的酶活性和细胞活性。 | |||
T6311 |
Bafetinib
NS-187,巴氟替尼,INNO-406 |
Bcr-Abl; Src; Autophagy | Angiogenesis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Bafetinib (INNO-406) 是一种特异性双重 Bcr-Abl/Lyn 抑制剂,IC50值为5.8和19 nM。 | |||
T7371 |
1-Naphthyl PP1 hydrochloride
1-叔丁基-3-(1-萘基)-1H-吡唑并[3,4-D]嘧啶-4-胺盐酸盐,1-NA-PP 1 hydrochloride |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) 是选择性的 src 家族激酶抑制剂,能够抑制 v-Src (IC50:1.0 μM)、c-Fyn (IC50:0.6 μM)、c-Abl (IC50:0.6 μM)、CDK2 (IC50:18 μM)、CAMK II (IC50:22 μM)。 | |||
T2293 |
SGX-523
|
Raf; p38 MAPK; c-Met/HGFR; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors |
SGX523 是选择性的和 ATP 竞争性的MET 抑制剂 (IC50:4 nM)。它对 MET 的选择性其它他蛋白激酶高 1000 倍。它具有抗肿瘤特性。 | |||
T2640 |
Rebastinib
DCC2036,DCC 2036,DCC-2036 |
Apoptosis; FLT; Bcr-Abl; Src | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Rebastinib (DCC-2036) 是一种口服有效的,非 ATP 竞争性的 Bcr-Abl 抑制剂,作用于 Abl1WT 和 Abl1T315I,IC50分别为 0.8 nM 和 4 nM,还抑制 LYN、SRC、HCK、FGR、FLT3、KDR 和 Tie-2,对 c-Kit 的活性低。Rebastinib 对 Angiopoietin2-Tie2通路具有抑制作用。 | |||
T4014 |
CP-724714
CP724714,CP 724714 |
Apoptosis; EGFR | Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
CP-724714 (CP724714) 是一种高效、选择性口服活性的 ErbB2 (HER2)酪氨酸激酶抑制剂,IC50为 10 nM。它能抑制完整细胞中 ErbB2 受体的自磷酸化,具有抗肿瘤活性。它对 EGFR 激酶有明显的选择性,IC50值为6400 nM。 | |||
T6079 |
NVP-ADW742
ADW742,ADW,GSK 552602A |
Apoptosis; IGF-1R | Apoptosis; Tyrosine Kinase/Adaptors |
NVP-ADW742 (ADW) 是一种具有口服活性,选择性的IGF-1R 酪氨酸激酶抑制剂,IC50为 0.17 μM。它抑制胰岛素受体,IC50为 2.8 μM,在肿瘤细胞中诱导多效性抗增殖/促凋亡。 | |||
T6277 |
Doramapimod
BIRB 796,达马莫德,度马莫德 |
Raf; p38 MAPK; Autophagy | Autophagy; MAPK |
Doramapimod (BIRB 796) 是一种具有口服活性的p38 MAPK 抑制剂,Kd 值为0.1nM。它也抑制B-Raf 和 Abl,IC50分别为 83 nM 和 14.6 μM。 | |||
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。 | |||
T67847 |
Imatinib impurities3
|
Bcr-Abl; PDGFR; c-Kit | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Imatinib impurities3是一种蛋白激酶抑制剂,对 ABL1 wt、KIT wt 和 PDGFRR wt 的 IC50值分别为6.95μM 、0.245μM 和0.139μM 。 | |||
T10801 |
CHMFL-ABL/KIT-155
CHMFL-ABL-KIT-155 |
c-Kit | Tyrosine Kinase/Adaptors |
CHMFL-ABL/KIT-155 is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s: 46 nM/75 nM). It arrests cell cycle progression and induces apoptosis. | |||
T1448L |
Dasatinib monohydrate
达沙替尼,BMS-354825 Monohydrate |
Apoptosis; Bcr-Abl; Src; c-Kit; Ephrin Receptor; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Dasatinib monohydrate (BMS-354825 Monohydrate) 是一种具有口服活性的,ATP 竞争性的双重Src/Bcr-Abl 抑制剂,有抗肿瘤活性,还诱导凋亡和自噬。它抑制Src 和Bcr-Abl 的IC50分别为 0.5 nM 和 <1.0 nM,Ki 值分别为 16 pM 和 30 pM。 | |||
T22303 |
Dasatinib hydrochloride
BMS-354825 HCl |
Bcr-Abl; Src; c-Kit | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Dasatinib hydrochloride (BMS-354825 HCl) (BMS-354825) hydrochloride 是一种具有口服活性的,ATP 竞争性的,双重 Src/Bcr-Abl 抑制剂,具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的 Ki 值分别为 16 pM 和 30 pM。Dasatinib hydrochloride hydrochloride 抑制 Bcr-Abl 和 Src 的IC50 分别为 <1.0 nM 和 0.5 nM。Dasatinib hydrochloride hydrochloride 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。 | |||
T83711 |
Abl Substrate Peptide TFA
|
||
Abl底物多肽是酪氨酸激酶Abl的多肽底物。在20 µM浓度下,相较于c-Src激酶,它被Abl选择性磷酸化。Abl底物多肽已被用于体外定量Abl激酶活性。 | |||
T11639 |
Imatinib D4
CGP-57148B D4,STI571 D4 |
Others | Others |
Imatinib D4 is a deuterium-labeled Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, PDGFR, v-Abl, and c-kit kinase activity. | |||
T27212 |
DSA-7
DSA7 |
||
DSA7 is a potent inhibitor of c-Src and Abl. | |||
T11640 |
Imatinib-d8
CGP-57148B D8,STI571 D8 |
Others | Others |
Imatinib D8 is a deuterium-labeled Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that inhibits BCR/ABL, PDGFR, v-Abl, and c-kit kinase activity. | |||
T40504 |
N-Desmethyl imatinib mesylate
ImatinibmetaboliteN-Desmethylimatinibmesylate,N-Desmethyl imatinib mesylate,Norimatinib mesylate |
||
Norimatinib mesylate, also known as N-Desmethyl imatinib mesylate, is a metabolite derived from Imatinib, which acts as a potent multi-target inhibitor of v-Abl, c-Kit, and PDGFR. | |||
T2116 |
AEE788
NVP-AEE 788 |
Apoptosis; EGFR; c-Fms; FLT; Bcr-Abl | Angiogenesis; Apoptosis; Cytoskeletal Signaling; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
AEE788 (NVP-AEE 788)是EGFR 和ErbB2的抑制剂,IC50值分别为2和6 nM。它已用于研究癌症、多形性胶质母细胞瘤以及脑和中枢神经系统肿瘤治疗的试验。 | |||
T22859 | Imatinib hydrochloride | Others | Others |
Imatinib is a multi-target inhibitor of v-Abl, c-Kit, and PDGFR (IC50: 0.6 μM, 0.1 μM, and 0.1 μM, respectively). Imatinib is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs), and a number of other malignancies. | |||
T23128 |
PD180970
PD 180970 |
Bcr-Abl; Src; c-Kit | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
PD180970 是一种 Bcr-Abl 抑制剂,对于 p210Bcr-Abl、Src 和 Kit 的自磷酸化,IC50 分别为 5 nM、0.8 nM 和 50 nM。 PD180970 可用于慢性粒细胞白血病的研究。 | |||
T73973 | Imatinib Impurity E | ||
Imatinib Impurity E 是 Imatinib 的杂质。Imatinib 是一种口服生物可用的酪氨酸激酶抑制剂,可选择性抑制 BCR/ABL,v-Abl,PDGFR,c-kit 激酶活性。Imatinib (STI571) 靠近 ATP 结合位点结合,将其锁定在封闭或自我抑制的构象中,因此半竞争性抑制蛋白质的酶活性。Imatinib 还抑制 SARS-CoV 和MERS-CoV。 | |||
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... | |||
T3641 |
NVP-BAW2881
BAW2881 |
Raf; VEGFR; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors |
NVP-BAW2881 (BAW2881) 是一种选择性的 VEGFR2抑制剂,其 IC50=9 nM。 | |||
T2609 |
Masitinib
AB1010,马赛替尼 |
Apoptosis; FAK; c-Fms; FGFR; Bcr-Abl; PDGFR; Src; c-Kit; Hck | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Masitinib (AB1010) 是生物口服可利用的选择性 c-Kit 抑制剂 (对于人重组c-Kit,IC50=200 nM),它还抑制PDGFRα/β(IC50s=540/800 nM),Lyn(对 LynB 的IC50=510 nM),Lck,较小程度上抑制FGFR3和FAK。它有抗增殖,促凋亡活性,且毒性低。 | |||
T1448 |
Dasatinib
BMS-354825,达沙替尼 |
Apoptosis; Bcr-Abl; Src; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Dasatinib (BMS-354825) 是一种酪氨酸激酶抑制剂,抑制 Src 和 Bcr-Abl (Ki=16/30 pM),具有口服活性和 ATP 竞争性。Dasatinib 具有抗肿瘤活性,用于治疗白血病和淋巴瘤等。 | |||
T2070 |
Agerafenib
RXDX-105,CEP 32496,CEP-32496,CEP32496 |
Raf; c-RET; Bcr-Abl; PDGFR; Src; c-Kit | Angiogenesis; Apoptosis; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors |
Agerafenib (CEP32496) 是口服高效的 BRAFV600E 抑制剂,Kd 为 14 nM。 | |||
T2372 |
Ponatinib
帕纳替尼,AP24534,普纳替尼 |
VEGFR; FGFR; Bcr-Abl; PDGFR; Src; c-Kit; Autophagy | Angiogenesis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Ponatinib (AP24534) 是一种有口服活性的多靶点激酶抑制剂,抑制Abl、PDGFRα、VEGFR2、FGFR1和Src 的IC50分别为 0.37 nM、1.1 nM、1.5 nM、2.2 nM 和 5.4 nM。 | |||
T21295 |
BIX02189
BIX 02189 |
ERK; MEK | MAPK |
BIX02189 是一种有效的选择性 MEK5 和 ERK5 抑制剂,IC50分别为 1.5 和 59 nM。 | |||
T1744 |
BIX02188
|
Apoptosis; MEK | Apoptosis; MAPK |
BIX02188 是一种具有选择性和有效性的 MEK5 抑制剂,抑制 MEK5 诱导表达致癌突变体FLT3-ITD的细胞凋亡。 | |||
T14928 |
Agerafenib hydrochloride
RXDX-105 hydrochloride,CEP-32496 (hydrochloride) |
c-RET; c-Kit | Apoptosis; Tyrosine Kinase/Adaptors |
Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM). |