Milciclib

Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.

Product Specifications

CAS Number

[802539-81-7]

Product Name Alternative

PHA-848125

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; CDK

Type

Reference compound

Related Pathways

Autophagy; Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PHA-848125.html

Purity

99.90

Solubility

DMSO : 20 mg/mL (ultrasonic)

Smiles

O=C(NC)C1=NN(C2=C1C(C)(CC3=CN=C(N=C23)NC4=CC=C(C=C4)N5CCN(CC5)C)C)C

Molecular Formula

C25H32N8O

Molecular Weight

460.57

Precautions

H302, H315, H319, H335

References & Citations

[1]Caporali S, Alvino E, Levati L, Esposito AI, Ciomei M, Brasca MG, Del Bufalo D, Desideri M, Bonmassar E, Pfeffer U, D'Atri S. Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhibitor PHA-848125. Biochem Pharmacol. 2012 Sep 1;84 (5) :598-611.|[2]Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M. Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy. Mol Cancer Ther. 2010 Aug;9 (8) :2243-54.|[3]Degrassi A, et al.  Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-Ras (G12D) LA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging. Mol Cancer Ther. 2010 Mar;9 (3) :673-81.|[4]Brasca, M.G., 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. 52 (16), 5152-5163 (2009) .