Milciclib | Multi CDK inhibitor

CAS:802539-81-7

Catalog Number:10-4867

Milciclib (802539-81-7) is a potent inhibitor of cyclin-dependent kinases (IC50s: CDK1 = 398 nM, CDK2 = 45 nM, 

CDK4 = 160 nM, CDK5 = 265 nM, CDK7 = 150 nM).1 It is also a potent inhibitor of TRKA and C (IC50 = A, 53 nM; C, 134 nM). 

Milciclib displayed antitumor activity across multiple cancer cell lines including lymphoma, colon, kidney, ovarian, NSCLC, 

neuroblastoma, and osteosarcoma.2 It was also active in various human cancer xenograft and other models. It showed 

antitumor activity in malignant glioma cells and acted synergistically with temozolomide.3  Milciclib displayed efficacy 

in combination with gemcitabine in patients with refractory solid tumors.4 It blocked glucose consumption in H460 and 

H1975 cells by decreasing SLC2A1 mRNA and protein levels and inhibiting glucose transport via CDK7 inhibition.5

802539-81-7, CDK inhibitor, CDK2 inhibitor, Milciclib, Milciclib supplier, Multi-CDK inhibitor, PHA-848125

CAS:802539-81-7

Catalog Number:10-4867

Activity:Multi CDK inhibitor

Chemical Names:N,1,4,4-Tetramethyl-8-[4-(4-methylpiperazin-1-yl)anilino]-5H-pyrazolo[4,3-h]quinazoline-3-carboxamide

Alternate Name:PHA-848125

Molecular Weight:460.59

Molecular Formula:C25H32N8O

Solubility:

Soluble in DMSO (20 mg/ml with warming)

Physical Properties:

Yellow solid

Purity:

>98% HPLC

NMR: (Conforms)

Storage Temperature:-20°C

Stability:Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.

Shipping Code:RT

References/Citations:

1.Brasca et al. (2009), Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyll]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 5152

2.Albanese et al. (2010); 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., 9 2243

3.Albanese et al. (2013); Anti-tumor efficacy on glioma models of PHA-848125, a multi-kinase inhibitor able to cross the blood-brain 

barrier, Br. J. Pharmacol., 169 156

4.Aspeslagh et al. (2017); Phase I dose-escalation study of milciclib in combination with gemcitabine in patients with refractory solid 

tumors, Cancer Chemother. Pharmacol., 79 1257

5.Ghezzi et al. (2019); A high-throughput screen identifies that CDK7 activates glucose consumption in lung cancer cells, Nat. Commun., 

10 5444

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