PARP/PI3K-IN-1

COA

级别和纯度:

≥98%

CAS编号: 2337386-47-5
分子式: C₃₃H₂₈F₄N₈O₃
分子量: 660.62
PubChem编号: 156588977

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货号 (SKU)	包装规格	是否现货
P647135-1mg	1mg	期货
P647135-5mg	5mg	期货
P647135-10mg	10mg	期货
P647135-25mg	25mg	期货

查看相关系列

Apoptosis (7108) Cell Cycle/DNA Damage (2603) DNA Damage (3514) Histone Modification (3105) PARP (124) PI3K (243) PI3K/Akt/mTOR (764) 表观遗传学 (1497)

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基本描述

规格或纯度	≥98%
英文名称	PARP/PI3K-IN-1
生化机理	PARP/PI3K-IN-1 （化合物 15）是一种强效 PARP/PI3K 抑制剂，对 PARP-1、PARP-2、PI3Kα、PI3Kβ、PI3Kδ 和 PI3Kγ 的 pIC 50 值分别为 8.22、8.44、8.25、6.54、8.13 和 6.08。PARP/PI3K-IN-1是一种高效的抗癌化合物，其靶标是
储存温度	-20°C储存
运输条件	超低温冰袋运输
作用类型	激活剂
产品介绍	PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC 50 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 In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: MDA-MB-468 cancer cells Concentration: 1 μM Incubation Time: 72 hours Result: Led to a significant increase in cell apoptosis. Western Blot AnalysisCell 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. In Vivo PARP/PI3K-IN-1 (i.p.; 50 mg/kg; twice daily (BID) for 34 consecutive days) significantly suppresses the tumor growth . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:PARP-1 8.22 (pIC 50 ) PARP-2 8.44 (pIC 50 ) PI3Kα 8.25 (pIC 50 ) PI3Kβ 6.54 (pIC 50 ) PI3Kδ 8.13 (pIC 50 ) PI3Kγ 6.08 (pIC 50 )
纯度	≥98%

名称和识别符

IIUPAC Name	4-[[3-[2-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-4-morpholin-4-yl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carbonyl]-4-fluorophenyl]methyl]-4H-phthalazin-1-one
INCHI	1S/C33H28F4N8O3/c34-25-6-5-18(14-26-19-3-1-2-4-20(19)31(46)43-42-26)13-22(25)32(47)45-8-7-21-27(17-45)40-29(41-30(21)44-9-11-48-12-10-44)23-16-39-28(38)15-24(23)33(35,36)37/h1-6,13,15-16,26H,7-12,14,17H2,(H2,38,39)
InChi Key	ZEXPYRCUAZYANY-UHFFFAOYSA-N
Smiles	C1CN(CC2=C1C(=NC(=N2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4)C(=O)C5=C(C=CC(=C5)CC6C7=CC=CC=C7C(=O)N=N6)F
PubChem CID	156588977
分子量	660.62

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