Milciclib | Multi CDK inhibitor

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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

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

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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

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