Pharmaceutical Chemical Pnu-159682 Powder for Research Only CAS: 202350-68-3

Pharmaceutical Chemical Pnu-159682 Powder for Research Only CAS: 202350-68-3


PNU-159682 Basic Info.
Product Name:PNU-159682 
CAS No.:202350-68-3
MW: 641.62
Molecule Formula: C32H35NO13
Purity :>98%
Solubility:DMSO
Mechanisms: Pathways:Cell Cycle/DNA Damage; Target:Topoisomerase
Pathways:Antibody-drug conjugates/ADCs Related; Target:ADCs cytotoxin
Biological Activity:
PNU-159682 is a major bioactive metabolite of Nemorubicin in human liver microsomes; > 3,000-foldcytotoxic than its parent compound(MMDX and doxorubicin).
IC50 value: 0.1-0.5 nM (HT-29; DU145; Jurkat cell lines, etc) [1]
Target: Topoisomerase I inhibitor



in vitro: The cytotoxicity of PNU-159682 were in the subnanomolar range (0.07-0.58 nmol/L) and noticeablylower than that recorded for both MMDX and doxorubicin; PNU-159682 was 2,360- to 790-fold and 6,420- to2,100-fold more potent than MMDX and doxorubicin, respectively
in vivo: An evaluation of the in vivo antitumor activity of PNU-159682, in comparison with that of MMDX, was
then conducted in mice bearing disseminated murine L1210 leukemia. Preliminary toxicity dose-finding
studies showed that 15 Ag/kg i.v. was the single-dose maximum tolerated dose of PNU-159682

The DNA alkylating mechanism of PNU-159682 (PNU), a highly potent metabolite of the anthracycline nemorubicin, was investigated by gel-electrophoretic, HPLC-UV, and micro-HPLC/mass spectrometry (MS) measurements. PNU quickly reacted with double-stranded oligonucleotides, but not with single-stranded sequences, to form covalent adducts which were detectable by denaturing polyacrylamide gel electrophoresis (DPAGE). Ion-pair reverse-phase HPLC-UV analysis on CG rich duplex sequences having a 5′-CCCGGG-3′ central core showed the formation of two types of adducts with PNU, which were stable and could be characterized by micro-HPLC/MS. The first type contained one alkylated species (and possibly one reversibly bound species), and the second contained two alkylated species per duplex DNA. The covalent adducts were found to produce effective bridging of DNA complementary strands through the formation of virtual cross-links reminiscent of those produced by classical anthracyclines in the presence of formaldehyde. Furthermore, the absence of reactivity of PNU with CG-rich sequence containing a TA core (CGTACG), and the minor reactivity between PNU and CGC sequences (TACGCG·CGCGTA) pointed out the importance of guanine sequence context in modulating DNA alkylation.



Pharmaceutical Chemical Pnu-159682 Powder for Research Only CAS: 202350-68-3

Related Products:

Q1: Have your Product Quality been Approved by Third Party Lab?
A: Yes, All products are strictly tested by our QC, confirmed by QA and approved by third party lab in China, USA, Canada, Germany, UK, Italy, France etc. So you will be assured with Good Quality if you choose us. 
 
Q2:How do you treat quality complaint?
A:First of all, our QC department will do strict examination of our export products by HPLC, UV, GC , 
TLC and so on in order to reduce the quality problem to near zero. If there is a real quality problem ,caused by us, we will send you free goods for replacement or refund your loss.
 
3. How to cooperate with us?
You can contact us for cooperation through the website contact information, or contact with the salesmen in our company. We will connect you about the specific detail via email. 

Q3: Do you Accept Sample Order?
A: Yes, we accept small order from 10g, 100g and 1kg for your evaluation quality of our goods.

Q4: Is there any discount?
A: Yes, for larger quantity, we always support with better price. 

Q5:Do you accept VISA business credit card ?
A:Sorry we don't accept VISA credit card,
we'd like to accept T/T  , Moneygram , Western Union.

Q6:How long does it take to the goods arrived ?
A:It is Depending on your location,
    For small order, please expect 5-7 days by DHL,UPS,TNT, FEDEX, EMS.
For mass order, please allow 5-8 days by Air, 20-35 days by Sea.

Q7  Do  you  have  any  reshipment  policy ?  
we have good after-sale service and re-shipment policy if the parcel  lose
Our long association with  our clients has brought great benefits
We always take the upmost care in the packaging of our products 
our clients will confirm this as even they struggle to find them without help at times.
But in spite of our best efforts it is still possible  will seize a small number of packages.
In this circumstance we promise reship free  to establish  long term relationship
 
Q8  How to proceed order?
Let me konw the items,quantity and the destination contury wihch help me to give you a right price
Please let me know the items you are looking for, quantity and the destination country.After you confirm all details of order, pay money 100% in advance and give us Shipping address.We arrange the shipment at first time after receive payment and offer after-sales service after you receive parcel.





Pharmaceutical Chemical Pnu-159682 Powder for Research Only CAS: 202350-68-3
  Pharmaceutical Chemical Pnu-159682 Powder for Research Only CAS: 202350-68-3


PNU-159682 Basic Info.
Product Name:PNU-159682 
CAS No.:202350-68-3
MW: 641.62
Molecule Formula: C32H35NO13
Purity :>98%
Solubility:DMSO
Mechanisms: Pathways:Cell Cycle/DNA Damage; Target:Topoisomerase
Pathways:Antibody-drug conjugates/ADCs Related; Target:ADCs cytotoxin
Biological Activity:
PNU-159682 is a major bioactive metabolite of Nemorubicin in human liver microsomes; > 3,000-foldcytotoxic than its parent compound(MMDX and doxorubicin).
IC50 value: 0.1-0.5 nM (HT-29; DU145; Jurkat cell lines, etc) [1]
Target: Topoisomerase I inhibitor



in vitro: The cytotoxicity of PNU-159682 were in the subnanomolar range (0.07-0.58 nmol/L) and noticeablylower than that recorded for both MMDX and doxorubicin; PNU-159682 was 2,360- to 790-fold and 6,420- to2,100-fold more potent than MMDX and doxorubicin, respectively
in vivo: An evaluation of the in vivo antitumor activity of PNU-159682, in comparison with that of MMDX, was
then conducted in mice bearing disseminated murine L1210 leukemia. Preliminary toxicity dose-finding
studies showed that 15 Ag/kg i.v. was the single-dose maximum tolerated dose of PNU-159682

The DNA alkylating mechanism of PNU-159682 (PNU), a highly potent metabolite of the anthracycline nemorubicin, was investigated by gel-electrophoretic, HPLC-UV, and micro-HPLC/mass spectrometry (MS) measurements. PNU quickly reacted with double-stranded oligonucleotides, but not with single-stranded sequences, to form covalent adducts which were detectable by denaturing polyacrylamide gel electrophoresis (DPAGE). Ion-pair reverse-phase HPLC-UV analysis on CG rich duplex sequences having a 5′-CCCGGG-3′ central core showed the formation of two types of adducts with PNU, which were stable and could be characterized by micro-HPLC/MS. The first type contained one alkylated species (and possibly one reversibly bound species), and the second contained two alkylated species per duplex DNA. The covalent adducts were found to produce effective bridging of DNA complementary strands through the formation of virtual cross-links reminiscent of those produced by classical anthracyclines in the presence of formaldehyde. Furthermore, the absence of reactivity of PNU with CG-rich sequence containing a TA core (CGTACG), and the minor reactivity between PNU and CGC sequences (TACGCG·CGCGTA) pointed out the importance of guanine sequence context in modulating DNA alkylation.



Pharmaceutical Chemical Pnu-159682 Powder for Research Only CAS: 202350-68-3

Related Products:

Q1: Have your Product Quality been Approved by Third Party Lab?
A: Yes, All products are strictly tested by our QC, confirmed by QA and approved by third party lab in China, USA, Canada, Germany, UK, Italy, France etc. So you will be assured with Good Quality if you choose us. 
 
Q2:How do you treat quality complaint?
A:First of all, our QC department will do strict examination of our export products by HPLC, UV, GC , 
TLC and so on in order to reduce the quality problem to near zero. If there is a real quality problem ,caused by us, we will send you free goods for replacement or refund your loss.
 
3. How to cooperate with us?
You can contact us for cooperation through the website contact information, or contact with the salesmen in our company. We will connect you about the specific detail via email. 

Q3: Do you Accept Sample Order?
A: Yes, we accept small order from 10g, 100g and 1kg for your evaluation quality of our goods.

Q4: Is there any discount?
A: Yes, for larger quantity, we always support with better price. 

Q5:Do you accept VISA business credit card ?
A:Sorry we don't accept VISA credit card,
we'd like to accept T/T  , Moneygram , Western Union.

Q6:How long does it take to the goods arrived ?
A:It is Depending on your location,
    For small order, please expect 5-7 days by DHL,UPS,TNT, FEDEX, EMS.
For mass order, please allow 5-8 days by Air, 20-35 days by Sea.

Q7  Do  you  have  any  reshipment  policy ?  
we have good after-sale service and re-shipment policy if the parcel  lose
Our long association with  our clients has brought great benefits
We always take the upmost care in the packaging of our products 
our clients will confirm this as even they struggle to find them without help at times.
But in spite of our best efforts it is still possible  will seize a small number of packages.
In this circumstance we promise reship free  to establish  long term relationship
 
Q8  How to proceed order?
Let me konw the items,quantity and the destination contury wihch help me to give you a right price
Please let me know the items you are looking for, quantity and the destination country.After you confirm all details of order, pay money 100% in advance and give us Shipping address.We arrange the shipment at first time after receive payment and offer after-sales service after you receive parcel.





Pharmaceutical Chemical Pnu-159682 Powder for Research Only CAS: 202350-68-3
 

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