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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P127815-1mg | 1mg | In stock | $56.90 | |
P127815-5mg | 5mg | In stock | $236.90 | |
P127815-10mg | 10mg | In stock | $391.90 | |
P127815-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $1,018.90 |
Potent, ATP-competitive CDK2 and TRKA inhibitor
Synonyms | DS-17315 | MMV676602 | SY034854 | NCGC00346673-01 | AC-35945 | AKOS030231455 | Milciclib; PHA 848125 | N,1,4,4-tetramethyl-8-[4-(4-methylpiperazin-1-yl)anilino]-5H-pyrazolo[4,3-h]quinazoline-3-carboxamide | SCHEMBL619139 | SR-05000022565 | PHA-848125,CAS: |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | PHA-848125 is an orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and thropomyosin receptor kinase A (TRKA), with potential antineoplastic activity.Potent, ATP-competitive CDK2/cyclin A (IC 50 = 45 nM) and Trk A inhibitor (IC 50 =\xa053 nM |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Nerve growth factor receptor Trk-A 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. |
ALogP | 2.8 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N,1,4,4-tetramethyl-8-[4-(4-methylpiperazin-1-yl)anilino]-5H-pyrazolo[4,3-h]quinazoline-3-carboxamide |
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INCHI | InChI=1S/C25H32N8O/c1-25(2)14-16-15-27-24(29-20(16)22-19(25)21(23(34)26-3)30-32(22)5)28-17-6-8-18(9-7-17)33-12-10-31(4)11-13-33/h6-9,15H,10-14H2,1-5H3,(H,26,34)(H,27,28,29) |
InChi Key | RXZMYLDMFYNEIM-UHFFFAOYSA-N |
Canonical SMILES | CC1(CC2=CN=C(N=C2C3=C1C(=NN3C)C(=O)NC)NC4=CC=C(C=C4)N5CCN(CC5)C)C |
Isomeric SMILES | CC1(CC2=CN=C(N=C2C3=C1C(=NN3C)C(=O)NC)NC4=CC=C(C=C4)N5CCN(CC5)C)C |
PubChem CID | 16718576 |
Molecular Weight | 460.57 |
CAS Registry No. | 802539-81-7 |
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PubChem CID | 16718576 |
ChEMBL Ligand | CHEMBL564829 |
RCSB PDB Ligand | P48 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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D2102156 | Certificate of Analysis | Jan 13, 2023 | P127815 |
D2102161 | Certificate of Analysis | Jan 13, 2023 | P127815 |
D2102162 | Certificate of Analysis | Jan 13, 2023 | P127815 |
D2102164 | Certificate of Analysis | Jan 13, 2023 | P127815 |
Solubility | DMSO 92 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
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1. Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R et al.. (2009) Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.. J Med Chem, 52 (16): (5152-63). [PMID:19603809] [10.1021/op500134e] |
2. Jorda R, Hendrychová D, Voller J, Řezníčková E, Gucký T, Kryštof V. (2018) How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem, 61 (20): (9105-9120). [PMID:30234987] [10.1021/op500134e] |