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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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
Synonyms | Dinaciclib|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 |
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Specifications & Purity | ≥98% |
Storage Temp | Store at -20°C |
Shipped In | Dry ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Cyclin-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. |
ALogP | 1.9 |
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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 |
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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 |
PubChem CID | 46926350 |
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Wikipedia | Dinaciclib |
CAS Registry No. | 779353-01-4 |
ChEMBL Ligand | CHEMBL2103840 |
Enter Lot Number to search for COA:
Solubility | DMSO: ≥ 56 mg/mL |
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Melt Point(°C) | 107-111°C |
Pictogram(s) | GHS08, GHS07 |
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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. |
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, 8 (11): (2360-5). [PMID:24007471] |