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Chemical Structure : PHA-848125
CAS No.: 802539-81-7
Catalog No.: PC-42578Not For Human Use, Lab Use Only.
Milciclib (PHA-848125) is a potent, selective, brain penetrant and orally available dual CDK and TRK inhibitor with IC50 of 45 and 53 nM for CDK2/cyclin A and TrkA, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $128 | In stock | |
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $528 | In stock | |
| 100 mg | Get quote |
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Milciclib (PHA-848125) is a potent, selective, brain penetrant and orally available dual CDK and TRK inhibitor with IC50 of 45 and 53 nM for CDK2/cyclin A and TrkA, respectively.
PHA-848125 shows cross-reactivity with other CDKs (CDK1/4/5/7), TrkB/C, Kit, Abl and PDGFR (IC50s<1 uM).
PHA-848125 inhibits cell proliferation of a wide panel of tumoral cell lines with submicromolar IC50.
PHA-848125 shows significant antitumor activity in various human xenografts.
| M.Wt | 460.5746 | |
| Formula | C25H32N8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]- |
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1. Brasca MG, et al. J Med Chem. 2009 Aug 27;52(16):5152-63.
2. Degrassi A, et al. Mol Cancer Ther. 2010 Mar;9(3):673-81.
3. Albanese C, et al. Mol Cancer Ther. 2010 Aug;9(8):2243-54.
4. Albanese C, et al. Br J Pharmacol. 2013 May;169(1):156-66.
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