Milciclib
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 202233

CAS#: 802539-81-7

Description: Milciclib, also known as PHA-848125 or PHA-848125AC, is an orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and thropomyosin receptor kinase A (TRKA), with potential antineoplastic activity. CDK2/TRKA inhibitor PHA-848125 AC potently inhibits cyclin-dependent kinase 2 (CDK2) and exhibits activity against other CDKs including CDK1 and CDK4, in addition to TRKA. Inhibition of these kinases may result in cell cycle arrest and apoptosis of tumor cells that express these kinases. CDKs are serine/threonine kinases involved in regulation of the cell cycle and may be overexpressed in some cancer cell types.


Chemical Structure

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Milciclib
CAS# 802539-81-7

Theoretical Analysis

MedKoo Cat#: 202233
Name: Milciclib
CAS#: 802539-81-7
Chemical Formula: C25H32N8O
Exact Mass: 460.26991
Molecular Weight: 460.57
Elemental Analysis: C, 65.19; H, 7.00; N, 24.33; O, 3.47

Size Price Shipping out time Quantity
50mg USD 450 2-3 months
100mg USD 750 2-3 months
200mg USD 1250 2-3 months
500mg USD 2250 2-3 months
1g USD 3250 2-3 months
2g USD 5650 2-3 months
Inquire bulk and customized quantity

Pricing updated 2021-03-09. Prices are subject to change without notice.

PHA-848125 is out of stock. We can make a new batch, lead time is about 2 months.

Synonym: PHA-848125; PHA848125; PHA 848125; PHA-848125AC; PHA 848125AC; PHA848125AC; Milciclib.

IUPAC/Chemical Name: N,1,4,4-tetramethyl-8-((4-(4-methylpiperazin-1-yl)phenyl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide

InChi Key: RXZMYLDMFYNEIM-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H32N8O/c1-25(2)14-16-15-27-24(29-20(16)22-19(25)21(23(34)26-3)30-32(22)5)28-17-6-8-18(9-7-17)33-12-10-31(4)11-13-33/h6-9,15H,10-14H2,1-5H3,(H,26,34)(H,27,28,29)

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

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Soluble in DMSO, not in water 100.0

Preparing Stock Solutions

The following data is based on the product molecular weight 460.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Degrassi A, Russo M, Nanni C, Patton V, Alzani R, Giusti AM, Fanti S, Ciomei M, Pesenti E, Texido G. 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. Epub 2010 Mar 2. PubMed PMID: 20197397.

2: Caporali S, Alvino E, Starace G, Ciomei M, Brasca MG, Levati L, Garbin A, Castiglia D, Covaciu C, Bonmassar E, D'Atri S. The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound. Pharmacol Res. 2010 May;61(5):437-48. Epub 2009 Dec 21. PubMed PMID: 20026273.

3: Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R, Fiorentini F, Isacchi A, Mercurio C, Moretti W, Panzeri A, Pastori W, Pevarello P, Quartieri F, Roletto F, Traquandi G, Vianello P, Vulpetti A, Ciomei M. Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-py razolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor. J Med Chem. 2009 Jul 15. [Epub ahead of print] PubMed PMID: 19603809.

4: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Apr;31(3):183-226. PubMed PMID: 19536362.  



Additional Information

Milciclib (PHA-848125) is a spectrum selective multi-kinase inhibitor of cyclin-dependent kinases initially identified in a CDK2 inhibitor project, as a potent inhibitor of the CDK2/Cyclin A complex. It possesses an unusual kinase inhibitory profile, being active also against other selected members of receptors tyrosine kinases, src family and splicing kinases. Uncontrolled cell proliferation is a hallmark of cancer cells. Alterations of the expression and/or genetic mutations of Cdks and other components of the pRB pathway, controlling the correct entry and progression through the cell cycle, were reported in more than 90% of human neoplasms.  Milciclib is currently in phase II as single agent in thymic carcinoma. (source: http://www.nervianoms.com/en/oncology-en/pipeline/milciclib.html).