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PHA-848125(Milciclib)

  Cat. No.:  DC7231   Featured
Chemical Structure
802539-81-7
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More than 5000 active chemicals with high quality for research!
Field of application
PHA-848125(Milciclib) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM; >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 802539-81-7
Chemical Name: (S)-2-(4-acetamidophenyl)-N-(5-isopropylthiazol-2-yl)propanamide
Synonyms: Milciclib; PHA 848125
SMILES: C[C@@H](C1=CC=C(NC(C)=O)C=C1)C(NC2=NC=C(C(C)C)S2)=O
Formula: C17H21N3O2S
M.Wt: 331.43
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Milciclib (PHA-848125) is a potent, 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.
In Vivo: Milciclib (PHA-848125; 5, 10, and 15 mg/kg, p.o.) inhibits the growth of tumor in 7,12-dimethylbenz(a) anthracene (DMBA)-induced rat mammary carcinoma model. Milciclib has significant antitumor activity in various human xenografts and carcinogen-induced tumors as well as in disseminated primary leukemia models, with plasma concentrations in rodents in the same range as those found active in inhibiting cancer cell proliferation[2]. Milciclib (PHA-848125; 40 mg/kg) induces a significant tumor growth inhibition in K-RasG12DLA2 mice, and this is accompanied by a reduction in the cell membrane turnover[3].
In Vitro: Milciclib (PHA-848125; 0.156 or 0.625 μM) up-regulates the expression of PDCD4, DDIT4, SESN2/sestrin 2 and DEPDC6/DEPTOR in GL-Mel cells[1]. Milciclib (PHA-848125) potently inhibits the kinase activity of CDK2/cyclin A complex and of TRKA in a biochemical assay, with IC50s of 45 and 53 nM, respectively. Milciclib induces a clear accumulation of cells in G1 phase. Milciclib strongly inhibits NGF-induced phosphorylation of TRKA in a dose-dependent manner[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC27001 SR-4835 SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13.
DC70595 MFH290 MFH290 (MFH-290) is a potent, highly selective, covalent inhibitor of CDK12/13 with IC50 of 25/49 nM.MFH290 forms a covalent bond with Cys-1039 of CDK12, and CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290.MFH290 exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes.MFH290 restored Pol II CTD phosphorylation and DNA damage repair gene expression AND augments the antiproliferative effect of the PARP inhibitor olaparib.
DC50184 dCeMM3 dCeMM3 (Compound 3) is a glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex.
DC49082 CDK5-IN-2 CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC50s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively.
DC44518 CDK7-IN-3 CDK7-IN-3 is a selective CDK7 inhibitor with a KD of 0.059 nM. CDK7-IN-3 shows poor inhibition on CDK2 (Ki=390 nM), CDK9 (Ki=290 nM), CDK12 (Ki=78 nM). CDK7-IN-3 induce apoptosis in tumor cells and has antitumor activity.
DC28661 Cdc7-IN-7 Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
DC28660 Cdc7-IN-6 Cdc7-IN-6 (compound I-D) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity.
DC28659 Cdc7-IN-5 Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
DC7493 SB1317(TG-02) SB1317(TG-02) is a novel small molecule potent CDK2/JAK2/FLT3 inhibitor with IC50s of 13/73/56 nM respectively.
DC11282 THZ2 THZ2 is a potent and selective CDK7 inhibitor with IC50 of 13.9 nM.
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