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Dinaciclib (SCH727965) - ≥98%, high purity , Cyclin-dependent kinase 9 inhibitor, CAS No.779353-01-4, Cyclin-dependent kinase 9 inhibitor

  • Moligand™
  • ≥98%
Item Number
D127362
Grouped product items
SKUSizeAvailabilityPrice Qty
D127362-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$88.90
D127362-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$400.90
D127362-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$652.90

Novel, potent, selective cyclin-dependent kinase (CDK) inhibitor

Basic Description

SynonymsDinaciclib|779353-01-4|SCH727965|Dinaciclib (SCH727965)|SCH 727965|SCH-727965|MK-7965|(S)-3-(((3-ethyl-5-(2-(2-hydroxyethyl)piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)methyl)pyridine 1-oxide|(2S)-1-[3-Ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]py
Specifications & Purity≥98%
Storage TempStore at -20°C
Shipped InDry ice
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionCyclin-dependent kinase 9 inhibitor
Product Description

Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation.
A novel and potent cyclin-dependent kinase inhibitor for Cdk2, Cdk5, Cdk1, and Cdk9

Product Properties

ALogP1.9

Associated Targets

CDK1 Tchem Cyclin-dependent kinase 1 10 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK13 Tchem Cyclin-dependent kinase 13 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ERCC2 Tchem General transcription and DNA repair factor IIH helicase subunit XPD 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHD4 Tchem Chromodomain-helicase-DNA-binding protein 4 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK9 Tchem Cyclin-dependent kinase 9 11 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK8 Tchem Cyclin-dependent kinase 8 4 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK4 Tclin Cyclin-dependent kinase 4 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 12 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK5 Tchem Cyclin-dependent-like kinase 5 10 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HSF1 Tchem Heat shock factor protein 1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKR1C3 Tchem Aldo-keto reductase family 1 member C3 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 2-[(2S)-1-[3-ethyl-7-[(1-oxidopyridin-1-ium-3-yl)methylamino]pyrazolo[1,5-a]pyrimidin-5-yl]piperidin-2-yl]ethanol
INCHI InChI=1S/C21H28N6O2/c1-2-17-14-23-27-19(22-13-16-6-5-9-25(29)15-16)12-20(24-21(17)27)26-10-4-3-7-18(26)8-11-28/h5-6,9,12,14-15,18,22,28H,2-4,7-8,10-11,13H2,1H3/t18-/m0/s1
InChi Key PIMQWRZWLQKKBJ-SFHVURJKSA-N
Canonical SMILES CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCCC4CCO
Isomeric SMILES CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCC[C@H]4CCO
PubChem CID 46926350
Molecular Weight 396.49

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

2 results found

Lot NumberCertificate TypeDateItem
L2325080Certificate of AnalysisJan 02, 2024 D127362
D1727044Certificate of AnalysisNov 16, 2022 D127362

Chemical and Physical Properties

SolubilityDMSO: ≥ 56 mg/mL
Melt Point(°C)107-111°C

Safety and Hazards(GHS)

Pictogram(s) GHS08,   GHS07
Signal Danger
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H372:Causes damage to organs through prolonged or repeated exposure

H340:May cause genetic defects

Precautionary Statements

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352:IF ON SKIN: wash with plenty of water.

P321:Specific treatment (see ... on this label).

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P260:Do not breathe dust/fume/gas/mist/vapors/spray.

P281:Use personal protective equipment as required.

P270:Do not eat, drink or smoke when using this product.

P362+P364:Take off contaminated clothing and wash it before reuse.

P203:Obtain, read and follow all safety instructions before use.

P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes.

P318:if exposed or concerned, get medical advice.

P337+P317:If eye irritation persists: Get medical help.

P332+P317:If skin irritation occurs: Get medical help.

P319:Get medical help if you feel unwell.

Related Documents

References

1. Beroukhim R, Mermel CH, Porter D, Wei G, Raychaudhuri S, Donovan J, Barretina J, Boehm JS, Dobson J, Urashima M et al..  (2010)  The landscape of somatic copy-number alteration across human cancers..  Nature,  463  (7283): (899-905).  [PMID:20164920]
2. Puyol M, Martín A, Dubus P, Mulero F, Pizcueta P, Khan G, Guerra C, Santamaría D, Barbacid M.  (2010)  A synthetic lethal interaction between K-Ras oncogenes and Cdk4 unveils a therapeutic strategy for non-small cell lung carcinoma..  Cancer Cell,  18  (1): (63-73).  [PMID:20609353]
3. Dean JL, McClendon AK, Hickey TE, Butler LM, Tilley WD, Witkiewicz AK, Knudsen ES.  (2012)  Therapeutic response to CDK4/6 inhibition in breast cancer defined by ex vivo analyses of human tumors..  Cell Cycle,  11  (14): (2756-61).  [PMID:22767154]
4. Choi YJ, Li X, Hydbring P, Sanda T, Stefano J, Christie AL, Signoretti S, Look AT, Kung AL, von Boehmer H et al..  (2012)  The requirement for cyclin D function in tumor maintenance..  Cancer Cell,  22  (4): (438-51).  [PMID:23079655]
5. Sawai CM, Freund J, Oh P, Ndiaye-Lobry D, Bretz JC, Strikoudis A, Genesca L, Trimarchi T, Kelliher MA, Clark M et al..  (2012)  Therapeutic targeting of the cyclin D3:CDK4/6 complex in T cell leukemia..  Cancer Cell,  22  (4): (452-65).  [PMID:23079656]
6. Zhang XH, Cheng Y, Shin JY, Kim JO, Oh JE, Kang JH.  (2013)  A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS..  Cancer Biol Ther,  14  (7): (597-605).  [PMID:23792647]
7. Martin MP, Olesen SH, Georg GI, Schönbrunn E.  (2013)  Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains..  ACS Chem Biol,  (11): (2360-5).  [PMID:24007471]

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