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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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。 | |||
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。 | |||
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 。 | |||
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. | |||
T19451 |
N-Desmethyl imatinib-d8
Norimatinib D8,Imatinib metabolite N-Desmethyl imatinib D8,N-Desmethyl imatinib D8 |
Others | Others |
N-Desmethyl imatinib D8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib. | |||
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. | |||
T19015 |
Imatinib Acid
|
Others | Others |
Imatinib Acid is usually used as a fluorescent probe or labeled chemical. | |||
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. | |||
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. | |||
T18592 |
Imatinib carbaldehyde
CGP-57148B carbaldehyde,STI571 carbaldehyde,PROTAC ABL binding moiety 1 |
Others | Others |
Imatinib carbaldehyde (also known as CGP-57148B carbaldehyde) is a compound derived from Imatinib, an inhibitor of the ABL protein. Imatinib carbaldehyde binds to the IAP ligand with the assistance of a linker, resulting in the formation of SNIPER[1]. | |||
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。 | |||
T64338 |
AKI603
AKI 603,AKI-603 |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
AKI603 是一种极光激酶 A 抑制剂,IC50值为 12.3 nM。它对白血病细胞具有很强的抗增殖活性,可用于克服白血病中 BCR-ABL-T315I 耐药性突变。 | |||
T3071 |
Olverembatinib
GZD 824 |
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Olverembatinib (GZD 824) 是一种高效的、口服具有活性的pan-Bcr-Abl 抑制剂,具有抗肿瘤活性。它能广泛而有效地抑制突变型 Bcr-Abl。它对天然的 Bcr-Abl 和 Bcr-AblT315I 作用的IC50值分别为 0.34 nM 和 0.68 nM。 | |||
T2429 |
Olverembatinib dimesylate
GZD824 Dimesylate,HQP1351 |
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Olverembatinib dimesylate (GZD824 Dimesylate) 是一种高效的、口服具有活性的pan-Bcr-Abl 抑制剂,具有抗肿瘤活性。它能广泛而有效地抑制突变型 Bcr-Abl。它对天然的 Bcr-Abl 和 Bcr-AblT315I 作用的IC50值分别为 0.34 nM 和 0.68 nM。 | |||
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。 | |||
T27555 |
HS-438
HS 438 |
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HS-438 inhibits imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia. | |||
T24496 |
MPT0B002
MPT-0-B-002,MPT 0 B 002 |
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MPT0B002 is a microtubule inhibitor that acts by downregulating T315I mutant Bcr-Abl and inducing apoptosis of imatinib-resistant chronic myeloid leukemia cells. | |||
T69045 |
ON012380
|
||
ON012380 is a non-ATP-competitive Bcr-Abl inhibitor, potently inhibiting imatinib-resistant Bcr-Abl mutants such as T315I. | |||
T23617 |
Aclacinomycin
Aclacinomycins,Siwenmycin |
||
Aclacinomycin A is an anthracycline drug. It sensitizes K562 chronic myeloid leukemia cells to imatinib through p38MAPK-mediated erythroid differentiation. It is used in the treatment of cancer. | |||
T18693 |
SNIPER(ABL)-049
|
Others | Others |
SNIPER(ABL)-049, conjugating Imatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 100 μM[1]. | |||
T71144 | Nilotinib N-oxide | ||
Nilotinib N-oxide is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia. | |||
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... | |||
T68338 | Nilotinib hydrochloride dihydrate | ||
Nilotinib hydrochloride dihydrate is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia. | |||
T71068 |
Nilotinib dihydrochloride dihydrate
|
||
Nilotinib dihydrochloride dihydrate is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia. | |||
T18694 |
SNIPER(ABL)-050
|
Others | Others |
SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker. This conjugation results in the reduction of BCR-ABL protein[1]. | |||
T18695 | SNIPER(ABL)-058 | Others | Others |
SNIPER(ABL)-058, conjugating Imatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM[1]. | |||
T61731 | PPARγ agonist 4 | ||
PPARγ agonist 4 (Compound 18b), a potent and selective PPARγ agonist, demonstrates antitumor efficacy only when used in conjunction with Imatinib. Notably, PPARγ agonist 4 does not exhibit cytotoxic effects on either non-resistant or resistant cells [1]. | |||
T61465 |
PPARγ agonist 3
|
||
PPARγ agonist 3, also known as Compound 18a, is a potent and selective agonist of PPARγ. This compound does not exhibit cytotoxicity towards both non-resistant and resistant cells. Notably, PPARγ agonist 3 demonstrates antitumor efficacy exclusively when co-administered with Imatinib [1]. | |||
T69296 |
PHA-680626
|
||
PHA-680626 is a potent and selective PLK inhibitor. PHA-680626 exhibits anti-proliferative and pro-apoptotic activity on Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ cells by inhibition of both Bcr-Abl tyrosine kinase and Aurora kinases. PHA-680626 inhibits Plk1 (IC50 = 0.53 μM), Plk2 (IC50 = 0.07 μM) and Plk3 (IC50 = 1.61 μM). | |||
T63450 |
BCR-ABL-IN-6
|
||
BCR-ABL-IN-6 (9h) 是一种伊马替尼衍生物,也是 Bcr-Abl 激酶的选择性抑制剂,能够作用于 Bcr-AblWT (IC50: 4.6 nM) 和 Bcr-AblT3151 (IC50: 277 nM)。BCR-ABL-IN-6 (9h)对 Bcr-Abl 激酶具有较强的细胞内亲和力 (EC50: 14.6 nM)。BCR-ABL-IN-6 (9h) 能够用于研究慢性髓细胞性白血病治疗。 | |||
T79711 |
Antitumor photosensitizer-4
|
Apoptosis | Apoptosis |
Antitumor photosensitizer-4 (compound 10b) 是靶向ABCG2酪氨酸激酶抑制剂(TKI)的有效代表,由达沙替尼与伊马替尼构成的光敏剂(PS)。该化合物能够诱发细胞凋亡(apoptosis)及ROS生成,在HepG2和B16-F10细胞上展现出显著的光毒性作用。 | |||
T71654 |
APcK110
|
||
APcK110 is a novel Kit inhibitor . APcK110 inhibits proliferation of the mastocytosis cell line HMC1.2 and the SCF-responsive cell line OCI/AML3 in a dose-dependent manner . APcK110 is a more potent inhibitor of OCI/AML3 proliferation than the clinically used Kit inhibitors imatinib and dasatinib and at least as potent as cytarabine. APcK110 inhibits the phosphorylation of Kit, Stat3, Stat5, and Akt in a dose-dependent fashion, showing activity of APcK110 on Kit and its downstream signaling path... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN4404 |
Ladanein
|
HCV Protease | Microbiology/Virology; Proteases/Proteasome |
Ladanein is a phytochemicals inhibitor that is known to disrupt the interactions of core and other hepatitis C virus (HCV) proteins.Ladanein possesses free radicals DPPH and ABTS +.scavenging activity, it also displays moderate (20-40 microM) activities against K562, K562R (imatinib-resistant), and 697 human leukemia cell lines. |