Azd2281 Potent Parp1 / Parp2 Inhibitor Olaparib CAS 763113-22-0

November 03, 2018

Model NO.: CAS 763113-22-0
Trademark: Quanao
Transport Package: Safe and Discreet Packing Ways
Specification: 10g/bag
Origin: Guangzhou China
HS Code: 2501001900
Model NO.: CAS 763113-22-0
Trademark: Quanao
Transport Package: Safe and Discreet Packing Ways
Specification: 10g/bag
Origin: Guangzhou China
HS Code: 2501001900
AZD2281  Potent PARP1 / PARP2 inhibitor Olaparib  CAS  763113-22-0

Olaparib (AZD2281, Ku-0059436)
AZD2281 Ku-0059436
Olaparib (AZD2281, Ku-0059436) is a selective PARP1 / 2 inhibitor with an IC50 of 5 nM / 1 nM in cell-free assays, 300-fold stronger than that of Tankyrase-1. Phase 3
Chemical Name : 4-(3-(1-(cyclopropanecarbonyl)piperazine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
CAS :763113-22-0
MF:    C24H23FN4O3
MW:    434.46
Solubility (25°C) : DMSO 86 mg/mL warming (197.94 mM) Water 0.002 mg/mL (0.0 mM) Ethanol <1 mg/mL
Stability :-20ºC Powder , 3 years : -80ºC Soluble in solvents 2years

Olapanil is a novel poly-ADP ribose polymerase (PARP) inhibitor, including PARP1, PARP2, and PARP3. PARP mediates a mechanism of DNA repair and plays an important role in DNA damage repair and cell apoptosis. Therefore, the mechanism of DNA damage repair by targeting to cells is mediated by PARP1 and PARCA2 mutant cancer cells Of the critical loopholes in the role, can be used for breast cancer susceptibility gene (BRCA) mutations, platinum-sensitive drug-resistant patients with recurrent severe ovarian cancer maintenance therapy.
A study by scientists at the Dana-Farber Cancer Institute at Harvard Medical School has found that the site of action of orapani is polymerase Q (POLQ, also known as POLθ). These scientists found that a large number of patients with ovarian cancer homologous recombination (homologous recombination, HR) repair pathway gene defective, and POLQ protein expression greatly increased, HR is an important repair DNA repair chain repair. They speculated that POLQ was intended to compensate for the loss of HR and to participate in DNA repair.
Experiments show that, HR normal cells, the knockout of POLQ HR activity will be significantly increased; and HR-deficient cells, knocking out POLQ can lead to cell death. POLQ containing RAD51 binding membrane, can block RAD51-mediated DNA repair. Related research published in the February 12, 2015, "Nature" on. Raphael Ceccaldi is the lead author of the study.
The study revealed that about 10% of ovarian cancer patients and 5% of breast cancer patients carrying BRCA1 or BRCA2 gene mutations, BRCA1 and BRCA2 belong to the tumor suppressor gene, HR repair pathway is the main component of their mutations mean HR repair pathway Missing. In cancer models of BRCA1 or BRCA2 mutations, PARP, a major component of the repair of single-stranded DNA breaks, can be synthesized to kill mutant cancer cells. Breeding of BRCA-deficient mice with POLQ-deficient mice resulted in embryonic death shortly after inoculation, which meant that there were two repair defects with embryonic lethality at the same time.
These findings suggest that the novel orally administered PARP inhibitor, which is able to kill BRCA-deficient cells, may be a cancer treatment for these carriers. Previously, the knowledge of BRCA mutations has not yet affected ovarian cancer or breast cancer treatment options, and after this study, it means that orapani can be used for BRCA1 or BRCA2 mutations in cancer patients targeted therapy, its The therapeutic target is a genetic defect in cancer cells rather than a target organ.
In ovarian cancer and breast cancer cells, BRCA mutations are the first hit of cell survival because it increases the susceptibility to DNA damage. By targeting the PARP-controlled backup and repair pathway, orapani and its analogous drugs achieved a second hit on cell survival. Accumulation of DNA damage has a third-hit effect on the cell as the two repair signaling pathways become unbalanced.


AZD2281 COA & HPLC :

Azd2281 Potent Parp1 / Parp2 Inhibitor Olaparib CAS 763113-22-0Azd2281 Potent Parp1 / Parp2 Inhibitor Olaparib CAS 763113-22-0Azd2281 Potent Parp1 / Parp2 Inhibitor Olaparib CAS 763113-22-0

Here Guangzhou Quanao chemical Co. Ltd is one of the worlds high-tech enterprise with completely independent intellectual property rights specialized in flavor, steroid powders , semi-finished steroid liquids , Sarm powders  , fragrance, chemical raw material, food additives, cinnamon series, plant extracts, pharmaceutical Products and high-quality powders for sale over several years. We offer you "safety, efficiency, Security" service. Get the service and products Here, we will offer you special discount. Any questions will be welcomed.


Relate Inhibitors products contact Bruce skype :angelo57434

ABT-888    
AZD2281    
GSK2126458    
BMS777607    
BMS5121458    
VX950    
Telatinib (BAY 57-9352)    
gsk1904529A    
LY2157299    
DMXAA(AS1404,ASA404)    
Brivanib(bms-540215)    
Brivanib alaninate(BMS-582664)    
vx-702    
abt-869    
NPS-2143    
AG014699    
AZD6244    
GSK1070916    
GSK1120212    
A-674563    
MLN8237    
AS605240    
YO01027    
PKI587    
LY2886721    
PF299804    
GSK690693    
PF-04691502    
SRT1720    
PP242    
KW-2478    
YM201636    
ms-275    
PI-103    
PKI-402    
GDC0980    
GSK1292263    
PHA665752    
LY573636    
AZD8055    
KU0063794    
MDV3100    
AST-1306    
Apixaban    
MGCD0103    
XL880    
MGCD265    
sns032    
ABT-263    
ABT-737    
NVP-BGJ398    
BAY73-4506    
Roflumilast,Daxas    
Fasudil hydrochloride    
Pelitinib(EKB-569)    
Neratinib(HKI-272)    
Imatinib    
Erlotinib HCL    
Afatinib(BIBW2992)    
PCI-32765    
AP24534(Ponatinib)    
AT101    
AZD5438    
CX-4945    
LY2109761    
RAF265    
LY294002    
KU55933    
XL184    
Linagliptin    
FUB359    
Canetinib    
Laquinimod    
Mastinib    
Torcetrapib    
Tasosartan    
A-803467    
JTC801    
Pyroxamide    
CP466722    
PF-562771    
TAK285    
ARN-509    
OC000459    
HQL-79    
JTT705    
MK-5108(VX689)    
LY2811376    
ctep    
PF-02341066    
TAK438    
IOX2    
GNF-2    
THIACETAZONE    
PD0325901    
R406    
AT-406    
R547    
CB-7598    
CB7630    
R788    
VU0364439    
TDZD-8    
VU 0361737    
TCS PIM-1 4a    
YS-49    
YM-90K hydrochloride    
PAI-039     
Dapivirine    
WZ 811     
TTP 22     
AG-490    
D-6413    
DY131    
GW 788388    
Merck-5 ,JAK INHIBITOR I     
JAK2 Inhibitor V  Z3    
KU14R     
LDN-211904    
MK 886    
TAC-101     
3-MA    
PHT427    
GW7647    
LY364947    
SB203580    
ZM323881    
ZM306416    
PF8380    
RITA (NSC 652287)    
ACY-1215    
ASP3026    
sch900776    
CP-945598    
OSI-027    
SB431542    
LY2623091    
Tenovin-1     
Apoptosis Activator 2     
HA14-1    
SMI-4a    
TWS119    
VU 0364439    
LY315920    
Anamorelin    
AZD2014    
LY2940680    
LY500307    
LY2608204    
TAK700    
Linagliptin(BI-1356)    
NVP-BHG712    
Amrubicin     
WAY362450    
AZD8931    
  AZD2281  Potent PARP1 / PARP2 inhibitor Olaparib  CAS  763113-22-0

Olaparib (AZD2281, Ku-0059436)
AZD2281 Ku-0059436
Olaparib (AZD2281, Ku-0059436) is a selective PARP1 / 2 inhibitor with an IC50 of 5 nM / 1 nM in cell-free assays, 300-fold stronger than that of Tankyrase-1. Phase 3
Chemical Name : 4-(3-(1-(cyclopropanecarbonyl)piperazine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
CAS :763113-22-0
MF:    C24H23FN4O3
MW:    434.46
Solubility (25°C) : DMSO 86 mg/mL warming (197.94 mM) Water 0.002 mg/mL (0.0 mM) Ethanol <1 mg/mL
Stability :-20ºC Powder , 3 years : -80ºC Soluble in solvents 2years

Olapanil is a novel poly-ADP ribose polymerase (PARP) inhibitor, including PARP1, PARP2, and PARP3. PARP mediates a mechanism of DNA repair and plays an important role in DNA damage repair and cell apoptosis. Therefore, the mechanism of DNA damage repair by targeting to cells is mediated by PARP1 and PARCA2 mutant cancer cells Of the critical loopholes in the role, can be used for breast cancer susceptibility gene (BRCA) mutations, platinum-sensitive drug-resistant patients with recurrent severe ovarian cancer maintenance therapy.
A study by scientists at the Dana-Farber Cancer Institute at Harvard Medical School has found that the site of action of orapani is polymerase Q (POLQ, also known as POLθ). These scientists found that a large number of patients with ovarian cancer homologous recombination (homologous recombination, HR) repair pathway gene defective, and POLQ protein expression greatly increased, HR is an important repair DNA repair chain repair. They speculated that POLQ was intended to compensate for the loss of HR and to participate in DNA repair.
Experiments show that, HR normal cells, the knockout of POLQ HR activity will be significantly increased; and HR-deficient cells, knocking out POLQ can lead to cell death. POLQ containing RAD51 binding membrane, can block RAD51-mediated DNA repair. Related research published in the February 12, 2015, "Nature" on. Raphael Ceccaldi is the lead author of the study.
The study revealed that about 10% of ovarian cancer patients and 5% of breast cancer patients carrying BRCA1 or BRCA2 gene mutations, BRCA1 and BRCA2 belong to the tumor suppressor gene, HR repair pathway is the main component of their mutations mean HR repair pathway Missing. In cancer models of BRCA1 or BRCA2 mutations, PARP, a major component of the repair of single-stranded DNA breaks, can be synthesized to kill mutant cancer cells. Breeding of BRCA-deficient mice with POLQ-deficient mice resulted in embryonic death shortly after inoculation, which meant that there were two repair defects with embryonic lethality at the same time.
These findings suggest that the novel orally administered PARP inhibitor, which is able to kill BRCA-deficient cells, may be a cancer treatment for these carriers. Previously, the knowledge of BRCA mutations has not yet affected ovarian cancer or breast cancer treatment options, and after this study, it means that orapani can be used for BRCA1 or BRCA2 mutations in cancer patients targeted therapy, its The therapeutic target is a genetic defect in cancer cells rather than a target organ.
In ovarian cancer and breast cancer cells, BRCA mutations are the first hit of cell survival because it increases the susceptibility to DNA damage. By targeting the PARP-controlled backup and repair pathway, orapani and its analogous drugs achieved a second hit on cell survival. Accumulation of DNA damage has a third-hit effect on the cell as the two repair signaling pathways become unbalanced.


AZD2281 COA & HPLC :

Azd2281 Potent Parp1 / Parp2 Inhibitor Olaparib CAS 763113-22-0Azd2281 Potent Parp1 / Parp2 Inhibitor Olaparib CAS 763113-22-0Azd2281 Potent Parp1 / Parp2 Inhibitor Olaparib CAS 763113-22-0

Here Guangzhou Quanao chemical Co. Ltd is one of the worlds high-tech enterprise with completely independent intellectual property rights specialized in flavor, steroid powders , semi-finished steroid liquids , Sarm powders  , fragrance, chemical raw material, food additives, cinnamon series, plant extracts, pharmaceutical Products and high-quality powders for sale over several years. We offer you "safety, efficiency, Security" service. Get the service and products Here, we will offer you special discount. Any questions will be welcomed.


Relate Inhibitors products contact Bruce skype :angelo57434

ABT-888    
AZD2281    
GSK2126458    
BMS777607    
BMS5121458    
VX950    
Telatinib (BAY 57-9352)    
gsk1904529A    
LY2157299    
DMXAA(AS1404,ASA404)    
Brivanib(bms-540215)    
Brivanib alaninate(BMS-582664)    
vx-702    
abt-869    
NPS-2143    
AG014699    
AZD6244    
GSK1070916    
GSK1120212    
A-674563    
MLN8237    
AS605240    
YO01027    
PKI587    
LY2886721    
PF299804    
GSK690693    
PF-04691502    
SRT1720    
PP242    
KW-2478    
YM201636    
ms-275    
PI-103    
PKI-402    
GDC0980    
GSK1292263    
PHA665752    
LY573636    
AZD8055    
KU0063794    
MDV3100    
AST-1306    
Apixaban    
MGCD0103    
XL880    
MGCD265    
sns032    
ABT-263    
ABT-737    
NVP-BGJ398    
BAY73-4506    
Roflumilast,Daxas    
Fasudil hydrochloride    
Pelitinib(EKB-569)    
Neratinib(HKI-272)    
Imatinib    
Erlotinib HCL    
Afatinib(BIBW2992)    
PCI-32765    
AP24534(Ponatinib)    
AT101    
AZD5438    
CX-4945    
LY2109761    
RAF265    
LY294002    
KU55933    
XL184    
Linagliptin    
FUB359    
Canetinib    
Laquinimod    
Mastinib    
Torcetrapib    
Tasosartan    
A-803467    
JTC801    
Pyroxamide    
CP466722    
PF-562771    
TAK285    
ARN-509    
OC000459    
HQL-79    
JTT705    
MK-5108(VX689)    
LY2811376    
ctep    
PF-02341066    
TAK438    
IOX2    
GNF-2    
THIACETAZONE    
PD0325901    
R406    
AT-406    
R547    
CB-7598    
CB7630    
R788    
VU0364439    
TDZD-8    
VU 0361737    
TCS PIM-1 4a    
YS-49    
YM-90K hydrochloride    
PAI-039     
Dapivirine    
WZ 811     
TTP 22     
AG-490    
D-6413    
DY131    
GW 788388    
Merck-5 ,JAK INHIBITOR I     
JAK2 Inhibitor V  Z3    
KU14R     
LDN-211904    
MK 886    
TAC-101     
3-MA    
PHT427    
GW7647    
LY364947    
SB203580    
ZM323881    
ZM306416    
PF8380    
RITA (NSC 652287)    
ACY-1215    
ASP3026    
sch900776    
CP-945598    
OSI-027    
SB431542    
LY2623091    
Tenovin-1     
Apoptosis Activator 2     
HA14-1    
SMI-4a    
TWS119    
VU 0364439    
LY315920    
Anamorelin    
AZD2014    
LY2940680    
LY500307    
LY2608204    
TAK700    
Linagliptin(BI-1356)    
NVP-BHG712    
Amrubicin     
WAY362450    
AZD8931    
 

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