Guangzhou Kafen Biotech Co.,Ltd
|Place of Origin:||China|
|Minimum Order Quantity:||As your required.|
|Packaging Details:||According to your requirements.|
|Delivery Time:||Within 24 hours after receiving your payment.|
|Payment Terms:||Western Union,Money Gram,Bank Transfer,Bitcoin|
MK-1775 Basic Info
|Alias||MK1775, MK 1775|
|Storage||store at 0-5 ℃|
|Packing Methods||designed disguised packing ways, 100% pass custom guarantee|
|Delivery time||within 18 hours after payment confirmed|
|Payment||T/T, Western Union,Money Gram , Bitcoin|
|Usage||MK-1775 is an inhibitor of the checkpoint kinase Wee1|
What is MK-1775?
MK-1775 is an inhibitor of the checkpoint kinase Wee1 (IC50 = 5.2 nM).1 It has been shown to inhibit the phosphorylation of Cdc2 at tryosine-15, which abrogates the G2 DNA damage checkpoint.1 In p53-deficient tumors that rely solely on the G2 checkpoint upon DNA damage, MK-1775, in combination with DNA-damaging chemotherapeutic agents, is reported to induce apoptosis in vitro and potentiate the inhibition of tumor growth in vivo.
MK-1775 treatment led to the inhibition of Wee1 kinase and reduced inhibitory phosphorylation of its substrate Cdc2. MK-1775, when dosed with gemcitabine, abrogated the checkpoint arrest to promote mitotic entry and facilitated tumor cell death as compared to control and gemcitabine treated tumors. MK-1775 monotherapy did not induce tumor regressions. However, the combination of gemcitabine with MK-1775 produced robust anti-tumor activity and remarkably enhanced tumor regression response (4.01 fold) compared to gemcitabine treatment in p53-deficient tumors. Tumor re-growth curves plotted after the drug treatment period suggest that the effect of the combination therapy is longer-lasting than that of gemcitabine. None of the agents produced tumor regressions in p53-wild type xenografts.
MK-1775 inhibits Wee1 kinase in an ATP-competitive manner. Compared to Wee1, MK-1775 displays 2- to 3-fold less potency against Yes with IC50 of 14 nM, 10-fold less potency against seven other kinases with >80% inhibition at 1 μM, and >100-fold selectivity over human Myt 1, another kinase that inhibits cyclin-dependent kinase 1 (CDC2) by phosphorylation at an alternative site (Thr14).
By abrogating the DNA damage checkpoint via blockade of Wee1 activity in WiDr cells bearing mutated p53, MK-1775 treatment inhibits the basal phosphorylation of CDC2 at Tyr15 (CDC2Y15) with EC50 of 49 nM, and suppresses gemcitabine-, carboplatin- or cisplatin-induced phosphorylation of CDC2 and cell cycle arrest in a dose-dependent manner, with EC50 of 82 nM and 81 nM, 180 nM and 163 nM, as well as 159 nM and 160 nM, respectively. MK-1775 treatment alone at 30-100 nM has no significant antiproliferative effect in WiDr and H1299 cells, whereas MK-1775 at 300 nM, sufficient to inhibit Wee1 by >80%, displays moderate but significant antiproliferative effects by 34.1% in WiDr cells and 28.4% in H1299 cells.
Shipping & Delivery
1.Packages are generally dispatched within approximately 2 days after receipt of payment.
2.After the each shipping we will provide you with:
1) a link & tracking number to track your package online.
2) the few pictures with your order & details.
3.About the Custom clearance,we packed in disguise ways.In our experience,the appropriate and safe delivery,there won't be problems.
4.We confirm 99% clearance,100% resending.
5.Is it the best & safest shipping for all our repeat customers!
Discreet packing ways as your requirement, 100% go through.
Store in cool and dry area and keep away from direct sunlight.oC
2 years, keep in formal storage condition.
We accept any Qty you require, grams to kilograms.
Samples Available, Contact now!
Top reason why you choose us ?
(1)Fast discreet delivery with great shipping success!
(2)Pictures with your order & details!
(3)We will provide you the tracking number!
(4)Keep track of your goods untill the goods are sent in to your hands.
(5)We confirm 99% clearance,100% resending.
(6)High quality,100% pure products!
(7)Delivery time approx.4-6 business days.
(8)Best, Safe and Secure services.
(9)Customer support 24/7.
Payment Methods:West Union,Moeny Gram, Bitcoin and Bank Transfer.
Delivery Ways:EMS,HKEMS,TNT,DHL,FedEX,UPS etc.
Shipment Time:Within 12 hours after confirmation of your payment
Other Service:Safe shipment,high purity and best price for you.