Determine the necessary mass, volume, or concentration for preparing a solution.
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 | 1-[3-ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2S-piperidineethanol | NSC800091 | NSC-800091 | 4V8ECV0NBQ | D09604 | HY-10492 | 2H-Pyran-2-one, tetrahydro-6-heptyl | DINACICLIB [INN] | SCH 727965 | SW220016-1 | 2-[(2S)-1-[ |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Dinaciclib(SCH 727965 ) is a pyrazolo[1,5-a]pyrimidine with potential antineoplastic activity. Dinaciclib(SCH 727965 ) selectively inhibits cyclin dependent kinases CDK1, CDK2, CDK5, and CDK9; inhibition of CDK1 and CDK2 may result in cell cycle repressio |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Cyclin-dependent kinase 9 inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |