Product Name :
PARP/PI3K-IN-1
Description:
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.
CAS:
2337386-47-5
Molecular Weight:
660.62
Formula:
C33H28F4N8O3
Chemical Name:
4-[(3-{2-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-4-(morpholin-4-yl)-5H,6H,7H,8H-pyrido[3,4-d]pyrimidine-7-carbonyl}-4-fluorophenyl)methyl]-1,4-dihydrophthalazin-1-one
Smiles :
NC1=CC(=C(C=N1)C1=NC(=C2CCN(CC2=N1)C(=O)C1=CC(CC2N=NC(=O)C3=CC=CC=C32)=CC=C1F)N1CCOCC1)C(F)(F)F
InChiKey:
ZEXPYRCUAZYANY-UHFFFAOYSA-N
InChi :
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)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 2337386-47-5|Molecular Weight: 660.62|Formula: C33H28F4N8O3|Chemical Name: 4-[(3-{2-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-4-(morpholin-4-yl)-5H,6H,7H,8H-pyrido[3,4-d]pyrimidine-7-carbonyl}-4-fluorophenyl)methyl]-1,4-dihydrophthalazin-1-one|Smiles: NC1=CC(=C(C=N1)C1=NC(=C2CCN(CC2=N1)C(=O)C1=CC(CC2N=NC(=O)C3=CC=CC=C32)=CC=C1F)N1CCOCC1)C(F)(F)F|InChiKey: ZEXPYRCUAZYANY-UHFFFAOYSA-N|InChi: 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)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Lycorine} web|{Lycorine} Metabolic Enzyme/Protease|{Lycorine} Biological Activity|{Lycorine} Formula|{Lycorine} manufacturer|{Lycorine} Autophagy} |Shelf Life: ≥12 months if stored properly.{{AZD1390} medchemexpress|{AZD1390} PI3K/Akt/mTOR|{AZD1390} TGF-beta/Smad|{AZD1390} Purity & Documentation|{AZD1390} In stock|{AZD1390} custom synthesis} |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:24487575 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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.|In Vivo:|PARP/PI3K-IN-1 (i.p.; 50 mg/kg; twice daily (BID) for 34 consecutive days) significantly suppresses the tumor growth.|Products are for research use only. Not for human use.|