PHA-848125 - ≥98%, high purity , Nerve growth factor receptor Trk-A inhibitor, CAS No.802539-81-7, Nerve growth factor receptor Trk-A inhibitor

Item Number

P127815

Grouped product items
SKU	Size	Availability	Price
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

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Basic Description

Synonyms	Milciclib\|PHA-848125\|802539-81-7\|PHA 848125\|Milciclib [INN]\|Milciclib (PHA-848125)\|UNII-688000M8S8\|PHA848125\|4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide\|N,1,4,4-tetramethyl-8-((4-
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.

Names and Identifiers

IUPAC Name	N,1,4,4-tetramethyl-8-[4-(4-methylpiperazin-1-yl)anilino]-5H-pyrazolo[4,3-h]quinazoline-3-carboxamide
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.

PubChem CID

ChEMBL Ligand

RCSB PDB Ligand

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4 results found

Lot Number	Certificate Type	Date	Item
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

References

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]
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]

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Basic Description