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CPI203,≥98% (HPLC)

别名:TEN010;JQ2;RG-6146;(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide;(S)-2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩[3,2-f][1,2,4]三唑[4,3-a][1,4]二氮杂-6-基)乙酰胺

CAS号 1446144-04-2 经验分子式(希尔表示法) C19H18ClN5OS 分子量 399.90 MDL number MFCD27997886 PubChem Substance ID 329825722 NACRES NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): SML1212
CAS号: 1446144-04-2
MDL号: MFCD27997886
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$322.30

产品描述

一种BRD4的抑制剂,IC50:37nM。

包装

5, 25 mg in glass bottle

Biochem/physiol Actions

CPI203 is an analog of the BET inhibitor (BETi) (+)-JQ1 and is bioavailable via oral or intraperitoneal administration.[1] It plays an important role in lenalidomide and dexamethasone functions in in vitro and in vivo models of multiple myeloma.[1] CPI203 inhibits proliferation, apoptosis and cell cycle arrest in A431 cell line and primary skin squamous cell carcinoma (SCC) cells.[2]

CPI203 is an inhibitor of BRD4, a bromodomain-containing protein that binds to histones to regulate recruitment of transcription factors. BRD4 is also an RNA Pol II kinase. CPI203 blocks BRD4 kinase activity in cells and in vivo. It has shown synergistic antitumor activity with lenalidomide in bortezomib-resistant mantle cell lymphoma.

性质

Quality Level  100
assay  ≥98% (HPLC)
form  powder
color  white to beige
solubility  DMSO: 20 mg/mL, clear
storage temp.  2-8°C
SMILES string  CC1=NN=C2[C@H](CC(N)=O)N=C(C3=CC=C(Cl)C=C3)C4=C(SC(C)=C4C)N21
InChI  1S/C19H18ClN5OS/c1-9-10(2)27-19-16(9)17(12-4-6-13(20)7-5-12)22-14(8-15(21)26)18-24-23-11(3)25(18)19/h4-7,14H,8H2,1-3H3,(H2,21,26)/t14-/m0/s1
InChI key  QECMENZMDBOLDR-AWEZNQCLSA-N


安全信息

RIDADR NONH for all modes of transport
WGK德国 WGK 3
商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16