021-51111890
购物车（）
sales@molnova.cn
PCI-29732
CAS No. 330786-25-9
PCI-29732 ( PCI29732 | PCI 29732 )
产品货号. M14102 CAS No. 330786-25-9
一种选择性且不可逆的 Btk 抑制剂，生化 Ki 为 8.2 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥581 | 有现货 |
|
| 10MG | ￥872 | 有现货 |
|
| 25MG | ￥1702 | 有现货 |
|
| 50MG | ￥2567 | 有现货 |
|
| 100MG | ￥3717 | 有现货 |
|
| 200MG | ￥5292 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥639 | 有现货 |
|
生物学信息
-
产品名称PCI-29732
-
注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
-
产品简述一种选择性且不可逆的 Btk 抑制剂，生化 Ki 为 8.2 nM。
-
产品描述A selective and irreversible Btk inhibitor with biochemical Ki of 8.2 nM; also inhibits Lck and Lyn with Ki of 4.6 and 2.5 nM.(In Vitro):PCI29732 shows cytotoxicity in different cells. The IC50 values are 7.94 μM for S1, 7.79 μM for S1-MI-80, 6.55 μM for H460, 6.34 μM for H460/MX20, 6.14 μM for KB, 6.02 μM for KBv200, 12.45 μM for HEK293/pcDNA3, 14.58 μM for HEK293-ABCG2-482-R2, and 13.24 μM for HEK293-ABCG2-482-T7 cells.PCI-29732 blocks the transcriptional up-regulation of a panel of B-cell activation genes in human CD20+ B cells stimulated at the B-cell antigen receptor (BCR).(In Vivo):PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 and enhances the anti-tumor efficacy of substrate chemotherapeutic agents.PCI 29732 (20 mg/kg; p.o.; every 3 d × 5 times) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice model.
-
体外实验PCI29732 shows cytotoxicity in different cells. The IC50 values are 7.94 μM for S1, 7.79 μM for S1-MI-80, 6.55 μM for H460, 6.34 μM for H460/MX20, 6.14 μM for KB, 6.02 μM for KBv200, 12.45 μM for HEK293/pcDNA3, 14.58 μM for HEK293-ABCG2-482-R2, and 13.24 μM for HEK293-ABCG2-482-T7 cells.PCI-29732 blocks the transcriptional up-regulation of a panel of B-cell activation genes in human CD20+ B cells stimulated at the B-cell antigen receptor (BCR).
-
体内实验PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 and enhances the anti-tumor efficacy of substrate chemotherapeutic agents.PCI 29732 (20 mg/kg; p.o.; every 3 d × 5 times) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice model. Animal Model:5-6 weeks old athymic nude mice (bearing H460/MX20 cells)Dosage:20 mg/kg (combination with Topotecan; every 3 d × 5 times, i.p., 3 mg/kg; topotecan was given 1 h after PCI29732 administration)Administration:P.o.; every 3 d × 5 times Result:Significant reductions in tumor weight and volume were observed in the group treated with PCI29732 in combination with Topotecan.
-
同义词PCI29732 | PCI 29732
-
通路Tyrosine Kinase
-
靶点BTK
-
受体BTK|Itk
-
研究领域Inflammation/Immunology
-
适应症——
化学信息
-
CAS Number330786-25-9
-
分子量371.435
-
分子式C22H21N5O
-
纯度>98% (HPLC)
-
溶解度DMSO: ≥ 53 mg/mL
-
SMILESNC1=C2C(N(C3CCCC3)N=C2C4=CC=C(OC5=CC=CC=C5)C=C4)=NC=N1
-
化学全称1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-cyclopentyl-3-(4-phenoxyphenyl)-
运输与储存
-
储存条件(-20℃)
-
运输条件With Ice Pack
-
稳定性≥ 2 years
参考文献
1. Pan Z, et al. ChemMedChem. 2007 Jan;2(1):58-61.
2. Honigberg LA, et al. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80.
产品手册
关联产品
-
Orelabrutinib
Orelabrutinib 是一种口服活性且不可逆的布鲁顿酪氨酸激酶 (BTK) 抑制剂。
-
PF-4989216
PF-4989216 是一种有效的选择性 PI3K 抑制剂，对 p110α、p110β、p110γ、p110δ 和 VPS34 的 IC50 分别为 2 nM、142 nM、65 nM、1 nM 和 110 nM。
-
BIIB068
BIIB068 是一种选择性、可逆且具有口服活性的 BTK 抑制剂（IC50 = 1 nM，Kd = 0.3 nM）。
