ChemicalBook > CAS DataBase List > PHA-848125

PHA-848125

Product Name
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
Formula Weight
460.57
MOL File
802539-81-7.mol
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PHA-848125 Property

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)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
21474
Product name
PHA-848125
Purity
≥98%
Packaging
1mg
Price
$62
Updated
2024/03/01
Cayman Chemical
Product number
21474
Product name
PHA-848125
Purity
≥98%
Packaging
5mg
Price
$135
Updated
2024/03/01
Cayman Chemical
Product number
21474
Product name
PHA-848125
Packaging
10mg
Price
$239
Updated
2024/03/01
TRC
Product number
P294490
Product name
PHA-848125
Packaging
2.5mg
Price
$130
Updated
2021/12/16
Usbiological
Product number
462344
Product name
PHA-848125
Packaging
2.5mg
Price
$425
Updated
2021/12/16
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PHA-848125 Chemical Properties,Usage,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 Suppliers

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802539-81-7, PHA-848125Related Search:

(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE MK-1775 Saracatinib BMS-265246 Flavopiridol (Alvocidib) HCl Olaparib MLN8054

  • 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