Contact us: +91 9550333722 040 - 40102781
Structured search
India
Choose your country
Different countries will display different contents
Try our best to find the right business for you.
My chemicalbook

Welcome back!

HomeProduct name listPHA-848125

PHA-848125

PHA-848125 Structural

What is PHA-848125?

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.

The Uses of PHA-848125

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.

What are the applications of Application

PHA-848125 is a potent, ATP-competitive Cdk2/cyclin A and Trk A inhibitor

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)

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.

Properties of PHA-848125

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)
color  Light yellow to yellow

Safety information for PHA-848125

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
Precautionary Statement Codes P280:Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for PHA-848125

Related products of tetrahydrofuran

You may like

  • 7726-95-6 Bromine 99.5% AR (4 x 500ml) 99%
    7726-95-6 Bromine 99.5% AR (4 x 500ml) 99%
    7726-95-6
    View Details
  • Formamide 99%
    Formamide 99%
    75-12-7
    View Details
  • 376608-65-0 2-[[(3Ar,4S,6R,6As)-6-Aminotetrahydro-2,2-Dimethyl-4H-Cy 99%
    376608-65-0 2-[[(3Ar,4S,6R,6As)-6-Aminotetrahydro-2,2-Dimethyl-4H-Cy 99%
    376608-65-0
    View Details
  • 2, 4-Pyrimidinediamine 3-Oxide 99%
    2, 4-Pyrimidinediamine 3-Oxide 99%
    74638-76-9
    View Details
  • 111974-72-2 99%
    111974-72-2 99%
    111974-72-2
    View Details
  • 85-81-4 6-Methoxy-8-Nitroquinoline 99%
    85-81-4 6-Methoxy-8-Nitroquinoline 99%
    85-81-4
    View Details
  • 3-Bromo-4,5-Dihydro-1H-Benzo[B]Azepin-2(3H)-One 99%
    3-Bromo-4,5-Dihydro-1H-Benzo[B]Azepin-2(3H)-One 99%
    86499-96-9
    View Details
  • (−)-Dip-Chloride 85116-37-6 99%
    (−)-Dip-Chloride 85116-37-6 99%
    85116-37-6
    View Details
Statement: All products displayed on this website are only used for non medical purposes such as industrial applications or scientific research, and cannot be used for clinical diagnosis or treatment of humans or animals. They are not medicinal or edible.