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PHA-848125

CAS No.
802539-81-7
Chemical Name:
PHA-848125
Synonyms
Milciclib;PHA-84812;PHA-848125;PHA-848125 USP/EP/BP;Milciclib (PHA-848125);PHA-848125 (Milciclib);4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h];N,1,4,4-tetramethyl-8-(4-(4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-
CBNumber:
CB92500952
Molecular Formula:
C25H32N8O
Molecular Weight:
460.57
MDL Number:
MFCD17169990
MOL File:
802539-81-7.mol
MSDS File:
SDS
Last updated:2023-06-08 09:02:50

PHA-848125 Properties

Melting point 190 °C
Density 1.33
storage temp. Store at -20°C
solubility ≥23.05 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
form solid
pka 14.44±0.40(Predicted)
FDA UNII 688000M8S8

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P280-P305+P351+P338
NFPA 704
0
2 0

PHA-848125 price More Price(27)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 21474 PHA-848125 ≥98% 802539-81-7 1mg $62 2024-03-01 Buy
Cayman Chemical 21474 PHA-848125 ≥98% 802539-81-7 5mg $135 2024-03-01 Buy
Cayman Chemical 21474 PHA-848125 802539-81-7 10mg $239 2024-03-01 Buy
TRC P294490 PHA-848125 802539-81-7 2.5mg $130 2021-12-16 Buy
Usbiological 462344 PHA-848125 802539-81-7 2.5mg $425 2021-12-16 Buy
Product number Packaging Price Buy
21474 1mg $62 Buy
21474 5mg $135 Buy
21474 10mg $239 Buy
P294490 2.5mg $130 Buy
462344 2.5mg $425 Buy

PHA-848125 Chemical Properties,Uses,Production

Description

PHA-848125 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) that potently inhibits Cdk2/cyclin A (IC50 = 45 nM). It is at least 3-fold less potent at Cdks 1, 3, 4, 5, and 7. PHA-848125 is orally available and displays efficacy in suppressing the growth of cancer cells or tumor xenografts in animals.

Uses

PHA-848125 is a cyclin dependent kinase (CDK) inhibitor. Oral PHA-848125 showed antitumor activity via dual targeting of cyclin-dependent kinase and tropomyosin receptor kinase families in human carcinoma cell and xenografted mouse model of carcinoma.

Enzyme inhibitor

This cyclin kinase-directed inhibitor (FW = 460.57 g/mol; CAS 802539-81- 7, 802540-32-5 (3HCl), 1253645-38-3 (Maleic acid); Solubility: 90 mg/mL DMSO; <1 mg/mL Water), systematically named N,1,4,4-tetramethyl-8-(4- (4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h] quinazoline-3-carboxamide, targets cyclin A/CDK2 inhibitor with IC50 of 45 nM. PHA-848125-treated cells show cell cycle arrest in G1 and reduced DNA synthesis, accompanied by inhibition of pRb phosphorylation and modulation of other CDK-dependent markers. Cyclin Target Selectivity: Cdk1 (weak, if any), Cdk2 (++), Cdk3 (weak, if any), Cdk4 (weak, if any), Cdk5 (weak, if any), Cdk6 (weak, if any), Cdk7 (weak, if any), Cdk8 (weak, if any), Cdk9 (weak, if any), Cdk10 (weak, if any)

target

CDK2/CyclinA

References

1. brasca mg, amboldi n, ballinari d et al. 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. 2009 aug 27;52(16):5152-63.

PHA-848125 Preparation Products And Raw materials

Raw materials

Preparation Products

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PHA-848125 4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide Milciclib PHA-848125 (Milciclib) Milciclib (PHA-848125) N,1,4,4-tetramethyl-8-(4-(4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide 4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide PHA 848125 4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h] PHA-84812 1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]- PHA-848125 USP/EP/BP 802539-81-7 Inhibitors