MK-1775

Catalog No.S1525

MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2.

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MK-1775 Chemical Structure

MK-1775 Chemical Structure
Molecular Weight: 500.6

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Product Information

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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2.
Targets Wee1 [1]
(Cell-free assay)
IC50 5.2 nM
In vitro 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. [1]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
ASPC-1Mn7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M4fIfmlEPTB;MUOuNkDDuSBzLkGg{txOM4C4WFI2PDV6OUW0
BxPC-3M4XBfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1TrdGlEPTB;MD64JOKyKDBwMEOg{txONH72S3YzPTR3OEm1OC=>
CFPAC-1M2nQOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFH4XppKSzVyPUOuN{DDuSByLkKg{txONIO1OGYzPTR3OEm1OC=>
HPACM3z3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NVruT|VtUUN3ME2wMlUhyrFiMD6wNUDPxE1?NHfIcpgzPTR3OEm1OC=>
MIAPaCa-2M2\HTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHv4XlNKSzVyPUCuOUDDuSByLkC1JO69VQ>?Mm\ENlU1PTh7NUS=
PANC-1MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{m0XmlEPTB;MUCuOkDDuSBzLkGg{txOMVSyOVQ2QDl3NB?=
SK-N-BE (2)M{XRNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NY[yO4Q3UUN3ME2yMlTjiIoEsfMAjVAvOyEQvF2=NYL1OFZXOjV|MEi5NVY>
SK-N-BE (2), PAN→MKMYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MmjnTWM2OD1{Nj625qCKyrIkgJm5MlYh|ryPNHPaeHozPTNyOEmxOi=>
SK-N-BE (2), MK→PANMmX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2XD[WlEPTB;Mj605qCKyrIkgJmwMlMh|ryPMkW3NlU{ODh7MU[=
SK-N-ASNUfEXmxGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M4LDS2lEPTB;MD61NQKBkcLz4pEJNE4xOiEQvF2=MWSyOVMxQDlzNh?=
SK-N-DZNHWxbIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXjlSVJ2UUN3ME2wMlM36oDLwsJihKkxNjBzIN88US=>NHj0RlkzPTNyOEmxOi=>
SK-N-ASNWHvUWI3SXCxcITvd4l{KEG|c3H5NF72cFU2ODBibl2=NU\4XVc5PDhiaB?=NG\mV5FqdmS3Y3XzJINmdGxiYYDvdJRwe2m|NXvkU5hwOjV|MEi5NVY>
SK-N-DZNYS4VmlKSXCxcITvd4l{KEG|c3H5MlnsOVAxKG6PMm\WOFghcA>?MoDnbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>?M3XaV|I2OzB6OUG2
THP-1NGC1XZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NUXFcZp{OTJ3L{K1NE82ODBibl2=MY[0PEBpM{nt[4lv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVzNWjMTYNGOjVyOES2NVQ>
MV4-11MmrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MUSxNlUwOjVyL{WwNEBvVQ>?Mn3qOFghcA>?M3n3d4lv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVzMlHoNlUxQDR4MUS=
U937MkjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NFj2SJQyOjVxMkWwM|UxOCCwTR?=MYK0PEBpNH;rPJdqdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>?NHe2RZMzPTB6NE[xOC=>
HL-60NFPLSmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmXHNVI2NzJ3MD:1NFAhdk1?MoLkOFghcA>?MlvNbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI>MV2yOVA5PDZzNB?=
OCI-AML3NHzYWoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MVixNlUwOjVyL{WwNEBvVQ>?MlPlOFghcA>?M2fCPYlv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVzMmr5NlUxQDR4MUS=
MOLM-13NVziNHZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M33IUlEzPS9{NUCvOVAxKG6PNHv0T2k1QCCqMlrVbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI>NX[zSoc{OjVyOES2NVQ>
CMKMkGzR4VtdCCYaXHibYxqfHliQYPzZZk>MW[xNE0yODByMDDuUS=>MofDO|IhcA>?MkPpdoVlfWOnczDj[YxtKH[rYXzpZol1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>?NYizTG1COjR7NkKzN|E>
CMYMlrtR4VtdCCYaXHibYxqfHliQYPzZZk>Mkn6NVAuOTByMECgcm0>NX;reVdLPzJiaB?=NVPKNJZyemWmdXPld{Bk\WyuII\pZYxq[mm2eTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6nch?=MkL6NlQ6PjJ|M{G=
DayoNX;UOXlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{n1fGlEPTB;MUWwJI5ONVi1[IlNOjR4NkG5NVA>
UW228NXe1[FNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MULJR|UxRTJ|MjDuUS=>MkHINlQ3PjF7MUC=
IST-MES1MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=>M16y[lE2OC9{NUCgcm0>M4nWNlczKGh?MnPp[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVzM1zKXFI1OzZ3N{iy
IST-MES2MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=>NFfqRZQyPTBxMkWwJI5ONEXQXYo4OiCqMWHlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI>NI\YUFIzPDN4NUe4Ni=>
RENMoTWR4VtdCCYaXHibYxqfHliQYPzZZk>NFLSe3YyPTBxMkWwJI5OMYC3NkBpNEWxO2NmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ?NVrS[IVCOjR|NkW3PFI>
NCI-H2452MnHpR4VtdCCYaXHibYxqfHliQYPzZZk>NEXrWVcyPTBxMkWwJI5ONV;jUJBUPzJiaB?=MWXlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI>M1K4cVI1OzZ3N{iy
MSTO-211HMoPXR4VtdCCYaXHibYxqfHliQYPzZZk>NEm2W20yPTBxMkWwJI5OMV63NkBpM4TYR4VvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>?NVfnbldtOjR|NkW3PFI>
NCI-H2052NXnGc5BDS2WubDDWbYFjcWyrdImgRZN{[Xl?NG[2fmoyPTBxMkWwJI5OMUK3NkBpMUDlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI>Mke1NlQ{PjV5OEK=
WEE1MmPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3foTmlEPTB;NT6yJI5OMoCzNlM3QTl4NUW=
CDC2M3PJ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEHDS|JKSzVy78{eNVAxOCCwTR?=MnXPNlM3QTl4NUW=
CDK7NFPKbVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1fxRmlEPTExvK6xNFAxKG6PM3jq[VI{Pjl7NkW1
MYT1MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1fkTGlEPTB;NUOwJI5ONH:z[|IzOzZ7OU[1OS=>
T98G MkXBRZBweHSxc3nzJGF{e2G7MWCxNFAwOjVyIH7NNVPWPYpGPiCqNUTmU4xX\W6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQh[2WubDDrbYxtcW6pM3KyXlIyQTl{N{mz
A549NEfPO5RCeG:ydH;zbZMhSXO|YYm=MVyyNFAhdk1?M3Hr[lEhcA>?NYXkSJkxemGmaX;z[Y5{cXSrenXzJG5US0yFIHPlcIx{KGmwIHGgdFU{NWSncHXu[IVvfCCvYX7u[ZI>M3HN[FIyPzl7MEOz
H460MXvBdI9xfG:|aYOgRZN{[Xl?MYWyNFAhdk1?NYflS|BxOSCqNWDwVWpVemGmaX;z[Y5{cXSrenXzJG5US0yFIHPlcIx{KGmwIHGgdFU{NWSncHXu[IVvfCCvYX7u[ZI>Mk[xNlE4QTlyM{O=
H1299MlP2RZBweHSxc3nzJGF{e2G7NHPyUZYzODBibl2=M2[2blEhcA>?M3nNTpJi\Gmxc3Xud4l1cXqnczDOV2NNSyClZXzsd{BqdiCjIIC1N{1l\XCnbnTlcpQhdWGwbnXyMYKyNVc6QTB|Mx?=
Calu-6 MmTBRZBweHSxc3nzJGF{e2G7M3;n[|IxOCCwTR?=NIm4dnIyKGh?NE\PZW5z[WSrb4PlcpNqfGm8ZYOgUnNEVENiY3XscJMhcW5iYTDwOVMu\GWyZX7k[Y51KG2jbn7ldi=>M3TZTlIyPzl7MEOz
WiDrMYLLbY5ie2ViQYPzZZl{MXWxNE0yODByMDDuUS=>NX\4[pZNQCCqM3i3folvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBETEN{IHH0JHR6ejF3IIfpeIgh[W5iRVO1NOKhfmGudXWgc4YhQDVibn3vcE9NKHC{ZYTy[YF1\WRid3n0bEBo\W2laYThZolv\Q>?NHfUV4MyQTh6N{W0OS=>

... Click to View More Cell Line Experimental Data

In vivo MK-1775 treatment alone at ~20 mg/kg displays minimal antitumor effects against WiDr xenografts in rats with T/C of 69% at day 3. Antitumor efficacy by MK-1775 alone in the nude rat HeLa-luc and TOV21G-shp53 xenograft models is also moderate. [1]
Features The first reported Wee1 inhibitor.

Protocol(Only for Reference)

Kinase Assay:

[1]

In vitro kinase assays Recombinant human Wee1 is used. Kinase reaction is conducted with 10 μM ATP, 1.0 μCi of [γ-33P]ATP, and 2.5 μg of poly(Lys, Tyr) as a substrate in the presence of increasing concentrations of MK-1775 at 30°C for 30 minutes. Radioactivity incorporated into the substrate is trapped on MultiScreen-PH plates and is counted on a liquid scintillation counter.

Cell Assay:

[1]

Cell lines WiDr, NCI-H1299, TOV21G, and HeLa
Concentrations Dissolved in DMSO, final concentrations ~10 μM
Incubation Time 24 hours
Method

Cells are treated with or without gemcitabine for 24 hours, then with MK-1775 for an additional 24 hours. Cell viability is determined with a WST-8 kit using SpectraMax. Cellular caspase-3/7 activities are determined with a Caspase-3/7 Glo kit.

Animal Study:

[1]

Animal Models Immunodeficient nude rats (F344/NJcl-rnu) bearing WiDr, HeLa-luc, or TOV21G-shp53 tumors
Formulation Prepared in a vehicle of 0.5% methylcellulose solution
Dosages ~20 mg/kg/day
Administration Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Hirai H, et al. Mol Cancer Ther, 2009, 8(11), 2992-3000.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02037230 Recruiting Adenocarcinoma of the Pancreas University of Michigan Cancer Center January 2014 Phase 1|Phase 2
NCT01827384 Recruiting Neoplasms National Cancer Institute (NCI)|National Institutes of He  ...more National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 2013 Phase 2
NCT01748825 Recruiting Neoplasms|Lymphoma National Cancer Institute (NCI)|National Institutes of He  ...more National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) November 2012 Phase 1
NCT01357161 Active, not recruiting Ovarian Cancer Merck Sharp & Dohme Corp. July 2011 Phase 2
NCT01164995 Recruiting Epithelial Ovarian Cancer The Netherlands Cancer Institute|Merck Sharp & Dohme Corp. July 2010 Phase 2

view more

Chemical Information

Download MK-1775 SDF
Molecular Weight (MW) 500.6
Formula

C27H32N8O2

CAS No. 955365-80-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 80 mg/mL (159.8 mM)
Water 0.0001 mg/mL (0.0 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 2% DMSO+30% PEG 300+5% Tween+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6-(4-(4-methylpiperazin-1-yl)phenylamino)-1,2-dihydropyrazolo[3,4-d]pyrimidin-3-one

Customer Product Validation(5)


Click to enlarge
Rating
Source Cancer Letters, 2015, 356(200): 656–668 . MK-1775 purchased from Selleck
Method H&E Staining
Cell Lines Mice bearing BxPC-3 xenograft tumors
Concentrations 20 mg/kg
Incubation Time 3 weeks
Results Individual drug treatment resulted in increased tumor necrosis, which was further increased following combination treatment, as indicated by H&E staining.

Click to enlarge
Rating
Source J Hematol Oncol 2014 7:53. MK-1775 purchased from Selleck
Method Western blot
Cell Lines AML, HL-60, HL-60/Ara-C cells
Concentrations 125, 250, 500 uM
Incubation Time 48 h
Results There was a concentration-dependent increase in apoptotic cells for the HL60/Ara-C cell line, whereas the parental cell line remained relatively unaffected by MK-1775 concentrations up to 500 nM. A concentration-dependent decrease in p-CDK1 and p-CDK2 accompanied by increase of γH2AX was detected in cells from patient AML#10 as well as in HL60/Ara-C. HL60 cells treated with 500 nM MK-1775 had a small increase of γH2AX and no change in p-CDK1 or p-CDK2, probably due to very low levels of expression prior to drug treatment.

Click to enlarge
Rating
Source Endocrinology 2013 154(9), 3219-27. MK-1775 purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations 1 uM
Incubation Time 2 h
Results To examine how ERK is activated in T47D cells, specific inhibitors of JAK2 (AZD1480) and EGFR (AG1478) were used. It found that pharmacological blockade of either EGFR or JAK2 reduced the phosphorylation of both STAT5 and ERK by GH.

Click to enlarge
Rating
Source PLoS One 2013 8(3), e57523. MK-1775 purchased from Selleck
Method Histopathological assessment
Cell Lines
Concentrations 30 mg/kg
Incubation Time 48 h
Results Additionally, the tumor cells in the MK-1775 alone and MK-1775+ gemcitabine groups exhibited increased cell size with abundant eosinophilic cytoplasm and significant osteoid production, consistent with differentiation. tumors treated with MK-1775 alone and with MK-1775+ gemcitabine had an increased Ki67 index of 73% and 79%. In the vehicle-and gemcitabine-treated tumors, caspase activity was observed in 2% and 6% of tumor cells, respectively. Despite the lack of apoptotic cell death, gemcitabine-treated tumors revealed a significant increase (96%) in γH2AX immunoreactivity compared to the control groups, demonstrating that treatment causes DNA damage but fails to induce cytotoxic response.

Click to enlarge
Rating
Source Oncol Rep 2014 32(5), 1991-8. MK-1775 purchased from Selleck
Method Immunofluorescence
Cell Lines HT29 cells
Concentrations 1 uM
Incubation Time 2 h
Results HT29 cells were treated with the indicated doses of AZD1480 for 2 h prior to the 2 h stimulation with IL-6. The cells were fixed and stained by the anti-phosphorylated STAT3 primary antibody and the FITC-conjugated secondary antibody. The nucleus was stained with DAPI. Figure shows that phosphorylated STAT3 and non-activated STAT3 are almost located in the cytoplasm instead of the nucleus. Thus, STAT3 translocates to the nucleus when activated.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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