SML2394
AT9283
≥98% (HPLC)
别名:
1-Cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea, AT 9283, AT-9283, N-Cyclopropyl-N′-[3-[6-(4-morpholinylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]-urea
登录 查看组织和合同定价。
选择尺寸
关于此项目
经验公式（希尔记法）:
C19H23N7O2
化学文摘社编号:
分子量:
381.43
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
AT9283, ≥98% (HPLC)
SMILES string
[nH]1nc(c(c1)NC(=O)NC5CC5)c2[nH]c3c(n2)ccc(c3)CN4CCOCC4
InChI
1S/C19H23N7O2/c27-19(21-13-2-3-13)24-16-10-20-25-17(16)18-22-14-4-1-12(9-15(14)23-18)11-26-5-7-28-8-6-26/h1,4,9-10,13H,2-3,5-8,11H2,(H,20,25)(H,22,23)(H2,21,24,27)
InChI key
LOLPPWBBNUVNQZ-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Biochem/physiol Actions
A multitargeted kinase inhibitor with in vivo anticancer efficacy and potent activity against Abl, aurora kinase A/B and JAK2/3.
AT9283 has also been shown to accelerate growth arrest in various xenograft models.
AT9283 is an ATP site-targeting pyrazole-benzimidazole-based molecule with inhibitory potency against multiple kinases, most notably Aurora A/B (IC50 ≤3.0 nM), JAK2/3 (IC50 = 1.2/1.1 nM), Abl T315I (IC50 = 4 nM), GSK3β, FGFR2, VEGFR3 (Flt4), Mer, Ret, Rsk2/3, Tyk2, Yes (IC50 = 1-10 nM). AT9283 also inhibits 72 other kinases/mutations at a reduced potency (IC50 = 10-30 nM against 14, 30-100 nM against 21, 100-300 against 37 targets), while displaying an IC50 >300 nM toward 144 other kinase targets. AT9283 inhibits the growth/survival of multiple solid tumor cell lines in vitro (IC50 = 7.7-20 nM) and shows anti-cancer efficacy in mice via i.p. injection in vivo (67% and 76%HCT116 tumor growth inhibition on day 16, respectively, with 15 and 20 mg/kg b.i.d., two-day on and two-day off; >95% inhibition of Ba/F3 ETV6-JAK2 leukemia proliferation on day 12 with 10 mg/kg b.i.d. on days 2–5 and 8–12).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Mark A Dawson et al.
British journal of haematology, 150(1), 46-57 (2010-05-29)
Constitutive activation of Janus kinase (Jak) 2 is the most prevalent pathogenic event observed in the myeloproliferative disorders (MPD), suggesting that inhibitors of Jak2 may prove valuable in their management. Inhibition of the Aurora kinases has also proven to be
Sanne H Olesen et al.
ChemMedChem, 11(11), 1137-1144 (2016-05-03)
Increasing evidence suggests key roles for members of the mammalian Sterile20-like (MST) family of kinases in many aspects of biology. MST3 is a member of the STRIPAK complex, the deregulation of which has recently been associated with cancer cell migration
Fiona J Sorrell et al.
Structure (London, England : 1993), 24(3), 401-411 (2016-02-09)
The highly diverse Numb-associated kinase (NAK) family has been linked to broad cellular functions including receptor-mediated endocytosis, Notch pathway modulation, osteoblast differentiation, and dendrite morphogenesis. Consequently, NAK kinases play a key role in a diverse range of diseases from Parkinson's
Targeting Protein Kinases for Cancer Therapy (2011)
Ruriko Tanaka et al.
Blood, 116(12), 2089-2095 (2010-06-16)
Despite promising clinical results from imatinib mesylate and second-generation ABL tyrosine kinase inhibitors (TKIs) for most BCR-ABL(+) leukemia, BCR-ABL harboring the mutation of threonine 315 to isoleucine (BCR-ABL/T315I) is not targeted by any of these agents. We describe the in
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持