021-51111890
购物车（）
sales@molnova.cn
PARP,PI3K-IN-1
CAS No. 2337386-47-5
PARP,PI3K-IN-1 ( —— )
产品货号. M33055 CAS No. 2337386-47-5
PARP/PI3K-IN-1 (compound 15) 是一种有效的 PARP/PI3K 抑制剂，对 PARP-1，PARP-2，PI3Kα，PI3Kβ，PI3Kδ 和 PI3Kγ 的 pIC50 值分别为 8.22、8.44、8.25、6.54、8.13、6.08。PARP/PI3K-IN-1 是针对多种肿瘤疾病的高效抗癌化合物。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥1131 | 有现货 |
|
| 10MG | ￥1834 | 有现货 |
|
| 25MG | ￥3608 | 有现货 |
|
| 50MG | ￥5143 | 有现货 |
|
| 100MG | ￥6768 | 有现货 |
|
| 200MG | ￥8883 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
-
产品名称PARP,PI3K-IN-1
-
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PARP/PI3K-IN-1 (compound 15) 是一种有效的 PARP/PI3K 抑制剂，对 PARP-1，PARP-2，PI3Kα，PI3Kβ，PI3Kδ 和 PI3Kγ 的 pIC50 值分别为 8.22、8.44、8.25、6.54、8.13、6.08。PARP/PI3K-IN-1 是针对多种肿瘤疾病的高效抗癌化合物。
-
产品描述PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.
-
体外实验PARP/PI3K-IN-1 (compound 15; 1 μM; 72 hours) leads to a significant increase in cell apoptosis. PARP/PI3K-IN-1 (1 μM; 72 hours) reduces the autophosphorylation levels of AKT and S6 while increases the autophosphorylation level of ERK after treating cells, indicating that it can inhibit the PI3K pathway and activate the ERK pathway. PARP/PI3K-IN-1 (1 μM) displays a strong capability to downregulate the expression of BRCA1/2 at the mRNA level in MDA-MB-468 cancer cells. PARP/PI3K-IN-1 not only shows significant inhibitory activity against BRCA-deficient cells HCC1937 and HCT116, but also displays potent anti-proliferative activity against BRCA-proficient cells MDA-MB-231 and MDA-MB-468. Apoptosis Analysis Cell Line:MDA-MB-468 cancer cells Concentration:1 μM Incubation Time:72 hours Result:Led to a significant increase in cell apoptosis. Western Blot Analysis Cell Line:MDA-MB-468 cancer cells Concentration:1 μM Incubation Time:72 hours Result:Reduced the autophosphorylation levels of AKT and S6 while increased the autophosphorylation level of ERK after treating cells.
-
体内实验PARP/PI3K-IN-1 (i.p.; 50 mg/kg; twice daily (BID) for 34 consecutive days) significantly suppresses the tumor growth.Animal Model:Six-week-old male BALB/c nude mice with MDA-MB-468 cells Dosage:50 mg/kg Administration:i.p.; twice daily (BID) for 34 consecutive days Result:Significantly suppressed the tumor growth.
-
同义词——
-
通路PI3K/Akt/mTOR signaling
-
靶点PI3K
-
受体PI3K | PARP
-
研究领域——
-
适应症——
化学信息
-
CAS Number2337386-47-5
-
分子量660.62
-
分子式C33H28F4N8O3
-
纯度>98% (HPLC)
-
溶解度In Vitro:?DMSO 中的溶解度 : 100 mg/mL (151.37 mM; 超声助溶 )
-
SMILESO=C1NN=C(C=2C=CC=CC12)CC3=CC=C(F)C(=C3)C(=O)N4CC5=NC(=NC(=C5CC4)N6CCOCC6)C7=CN=C(N)C=C7C(F)(F)F
-
化学全称——
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. Wang J, et al.Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.J Med Chem. 2020 Jan 9;63(1):122-139.?
产品手册
关联产品
-
AZD8186
AZD8186 是一种有效的异构体特异性 PI3Kβ 抑制剂，IC50 为 4 nM，还抑制 PI3Kδ (IC50=12 nM)，选择性高于 PI3Kα (IC50=35 nM) 和 PI3Kγ (IC50=675 nM)。
-
IHMT-PI3Kδ-372 S-iso...
IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer shows high selectivity over other class I PI3Ks (56～83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.
-
GNE-490
GNE-490 是一种有效的、选择性的、口服的 I 类 PI3K 抑制剂。
