Milciclib, CDK inhibitor (TBI4867)

Description

Product Details

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

Alternate Names: PHA-848125

Molecular Formula: C₂₅H₃₂N₈O

Formula Weight: 460.6

CAS Number: 802539-81-7

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (20 mg/ml with warming).

Storage: -20°C

Stability: ≥ 2 years

Applications

CDK inhibitor

Functions

Potent inhibitor of cyclin-dependent kinases (IC₅₀s: CDK1 = 398 nM, CDK2 = 45 nM, CDK4 = 160 nM, CDK5 = 265 nM, CDK7 = 150 nM). It is also a potent inhibitor of TRKA and C (IC₅₀ = A, 53 nM; C, 134 nM). Displayed antitumor activity across multiple cancer cell lines including lymphoma, colon, kidney, ovarian, NSCLC, neuroblastoma, and osteosarcoma. 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. Displayed efficacy in combination with gemcitabine in patients with refractory solid tumors. It blocked glucose consumption in H460 and H1975 cells by decreasing SLC2A1 mRNA and protein levels and inhibiting glucose transport via CDK7 inhibition.

Application Procedures

First dissolved in DMSO (20 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4867_Milciclib_datasheet

MSDS:

TBI4867_Milciclib_MSDS

Research use only.