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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T18595 |
Dasatinib carbaldehyde
PROTAC ABL binding moiety 4,BMS-354825 carbaldehyde |
Others; Ligands for Target Protein for PROTAC | Others; PROTAC |
Dasatinib carbaldehyde (PROTAC ABL binding moiety 4) 基于 ABL 抑制剂达沙替尼,通过接头与 IAP 配体结合,形成 SNIPER [1]。 | |||
T37600 |
Dasatinib N-oxide
|
Others; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Others; Tyrosine Kinase/Adaptors |
Dasatinib N-oxide 是 Dasatinib 的一种次要代谢物。Dasatinib 是口服有效的Src/Bcr-Abl 抑制剂。 | |||
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)。 | |||
T18750 |
N-Deshydroxyethyl Dasatinib
N-Deshydroxyethyl BMS-354825 |
Others; IAP; Drug Metabolite | Apoptosis; Metabolism; Others |
N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) 是 Dasatinib 的代谢物,是以达沙替尼为基础的分子,通过连接体与 IAP 配体结合,形成 SNIPER,从而降解 ABL。N-Deshydroxyethyl Dasatinib 可用于研究癌症和免疫疾病。 | |||
T37645 |
Dasatinib metabolite M6
达沙替尼羧酸 |
Others | Others |
Dasatinib metabolite M6 (Dasatinib carboxylic acid) is an oxidative metabolite of Dasatinib, a potent and orally active inhibitor of both Bcr-Abl and Src family tyrosine kinases[1]. | |||
T30540 |
BMS-748730
4′-Hydroxy Dasatinib,,Dasatinib metabolite M20 |
Others | Others |
BMS-748730, also known as 4′-Hydroxy Dasatinib, is a Dasatinib metabolite. | |||
T84687 |
Dasatinib analog-1
|
Others | Others |
Dasatinib Analog-1,其Ki值为5.4 μM,能够抑制CYP3A4活力,并能阻断谷胱甘肽加合物的形成。 | |||
T71581 |
SGX393
|
Others | Others |
SGX393 is an inhibitor of the CML mutant Bcr-AblT315I, thereby preempting in vitro resistance when combined with nilotinib or dasatinib. | |||
T18686 |
SNIPER(ABL)-019
|
Others | Others |
SNIPER(ABL)-019, conjugating Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM[1]. | |||
T18690 |
SNIPER(ABL)-039
|
Others | Others |
SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively[1]. | |||
T18687 |
SNIPER(ABL)-020
|
Others | Others |
SNIPER(ABL)-020 is a chemical compound consisting of Dasatinib, an ABL inhibitor, and Bestatin, an IAP ligand, conjugated with a linker. This compound effectively reduces the BCR-ABL protein[1]. | |||
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
|
Others | Others |
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... | |||
T83930 |
SJ 11646
|
Others | Others |
SJ11646是一种高效的LCK(淋巴细胞特异性蛋白酪氨酸激酶)降解剂(PROTAC;DC50= 0.00838 pM)。该化合物由Dasatinib作为LCK配体,以及基于苯基谷氨酰亚胺的cereblon结合体组成。它在体外对LCK激活的T细胞急性淋巴细胞白血病(T-ALL)细胞株和初级白血病样本展现出细胞毒性。在体内,SJ11646在源自患者的T-ALL异种移植模型中显示出抗白血病效果。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-04817 |
Syntenin Protein, Human, Recombinant (His)
MDA-9,SYCL,TACIP18,syndecan binding protein (syntenin),ST1,M... |
Human | E. coli |
Syntenin1/SDCBP (syndecan binding protein), also known as melanoma differentiation associated gene-9 (MDA-9), is a PDZ domain-containing molecule, which was initially identified as a key oncogene in melanoma. IL-6 promotes glioma cell proliferation and invasion by inducing SDCBP expression, which is mediated by JAK2/STAT3 signaling. SDCBP might be an important marker for identifying Triple negative breast cancer (TNBC) cases that are suitable for dasatinib therapy. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10962 |
Dasatinib-d8
BMS-354825 D8 |
Others | Others |
Dasatinib D8 is deuterium-labeled dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor. |