AMG 900

产品编号: DC9366 Featured
AMG 900
结构式
945595-80-2
此产品仅供科研所需,我们不出售给病人
​我们将匹配市场上最好的价格给您
Email:order@dcbio.cn
免费咨询电话:4008862077
我们的合作伙伴:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
中国地区超过5000个高品质化合物库存
应用领域
AMG 900 是一种有效的选择性的 pan-Aurora 激酶抑制剂,作用于 Aurora A,B 和 C,IC50 分别为 5 nM,4 nM 和 1 nM。
Cas No.: 945595-80-2
名称:
别名: AMG-900;AMG900
SMILES: CC1=CSC(C2=NN=C(C3=C2C=CC=C3)NC4=CC=C(C=C4)OC5=C(C=CC=N5)C6=CC=NC(N)=N6)=C1
分子式: C28H21N7Os
分子量: 503.5776
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM; >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2. in vitro: AMG 900 is a novel class of ATP-competitive phthalazinamine small molecule inhibitors of aurora kinases. In HeLa cells, AMG 900 inhibits autophosphorylation of aurora-A and -B as well as phosphorylation of histone H3 on Ser, a proximal substrate of aurora-B. The predominant cellular response of tumor cells to AMG 900 treatment is aborted cell division without a prolonged mitotic arrest, which ultimately results in cell death. AMG 900 inhibits the proliferation of 26 tumor cell lines, including cell lines resistant to the antimitotic drug paclitaxel and to other aurora kinase inhibitors (AZD1152, MK-0457, and PHA-739358), at low nanomolar concentrations (about 2- 3 nM). Furthermore, AMG 900 is active in an AZD1152-resistant HCT116 variant cell line that harbors an aurora-B mutation (W221L). in vivo: Oral administration of AMG 900 blocks the phosphorylation of histone H3 in a dose-dependent manner and significantly inhibited the growth of HCT116 tumor xenografts. AMG 900 is broadly active in multiple xenograft models, including 3 multidrugresistant xenograft models, representing 5 tumor types. AMG 900 exhibits a low-to-moderate clearance and a small volume of distribution. Its terminal elimination half-life ranged from 0.6 to 2.4 hours. AMG 900 is well-absorbed in fasted animals with an oral bioavailability of 31% to 107%. Food intake has an effect on rate (rats) or extent (dogs) of AMG 900 oral absorption. The clearance and volume of distribution at steady state in humans are predicted to be 27.3 mL/h/kg and 93.9 mL/kg, respectively. AMG 900 exhibits acceptable PK properties in preclinical species and is predicted to have low clearance in humans.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
TITLE DOWNLOAD
MSDS_2642_DC9366_945595-80-2
COA
LOT NO. DOWNLOAD
产品编号 产品名称 应用领域
DC9366 AMG 900 AMG 900 是一种有效的选择性的 pan-Aurora 激酶抑制剂,作用于 Aurora A,B 和 C,IC50 分别为 5 nM,4 nM 和 1 nM。
DC7070 AT9283 AT9283 是一种多靶点激酶抑制剂,有效抑制 Aurora A/B,JAK2/3,Abl (T315I),和 Flt3 (IC50 值范围为 1-30 nM)。AT9283 抑制多种实体瘤在体内外的生长和存活。
DC7060 AZD1152 (barasertib) AZD1152 是 Barasertib-hQPA 的前体药物,是高度选择性的 Aurora B 抑制剂,IC50 值为 0.37 nM。
DC4125 PHA-739358 (danusertib) Danusertib 是一种极光激酶 (aurora kinase) 抑制剂,能够抑制 Aurora A,Aurora B 和 Aurora C 的活性,IC50 值分别为 13,79 和 61 nM。
DC3106 VX-680 (MK-0457,Tozasertib) Tozasertib (VX 680; MK-0457) 是 Aurora A/B/C 激酶抑制剂,Ki 值分别为 0.6,18,4.6 nM。