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
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)
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.
N-Bromosuccinimide Price
- Product number
- 21474
- Product name
- PHA-848125
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 21474
- Product name
- PHA-848125
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $135
- Updated
- 2024/03/01
- Product number
- 21474
- Product name
- PHA-848125
- Packaging
- 10mg
- Price
- $239
- Updated
- 2024/03/01
- Product number
- P294490
- Product name
- PHA-848125
- Packaging
- 2.5mg
- Price
- $130
- Updated
- 2021/12/16
- Product number
- 462344
- Product name
- PHA-848125
- Packaging
- 2.5mg
- Price
- $425
- Updated
- 2021/12/16
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.