crozbaciclib free base · Synonyms: CDK4/6/1 Inhibitor

Crozbaciclib is a CDK4/6 inhibitor.

For research use only. Not for human or veterinary use.

Target CDK

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

crozbaciclib structure

CAS No.: 2099128-41-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 mg	USD 498.00	BP-01196-5mg	In stock	Get quote
10 mg	USD 789.00	BP-01196-10mg	In stock	Get quote
25 mg	USD 1,385.00	BP-01196-25mg	In stock	Get quote
50 mg	USD 1,885.00	BP-01196-50mg	In stock	Get quote
100 mg	Inquire	BP-01196-100mg	In stock	Inquire
250 mg	Inquire	BP-01196-250mg	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

Crozbaciclib (CDK4/6/1 Inhibitor) is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.

Biological activity

In Vitro Crozbaciclib is a potent anti-proliferative agent that arrests U87MG cell line exclusively in G1 (IC50=15.3 ± 2.9 nM in the anti-proliferation assay). Crozbaciclib (13.72 nM; 24 h) significantly increases in the percentage of cells in G1 in U87MG cells In Vivo Crozbaciclib (3.125-50 mg/kg; ) has tumor growth inhibition values ranging from 62% to 99% in an orthotopic xenograft mouse model of glioblastoma multiforme. And Crozbaciclib results insignificant body weight loss. Crozbaciclib increases life span based on the median survival time of vehicle-treated animals in mice is significant at 162%, at a dose of 50 mg/kg

Identifiers

SMILES: CC(C1(CCCC1)C2=CC(C3=NC(NC4=CC=C(C5CCN(C)CC5)C=N4)=NC=C3F)=C6)=NC2=C6F
InChIKey: AEFFENQISAXIKE-UHFFFAOYSA-N

Specifications

MW (average): 488.5748
Formula: C₂₈H₃₀F₂N₆
CAS No.: 2099128-41-1
Physical state: Solid
Color: off-white to yellow
Shipping: 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: Powder 4℃, 2 years; In solvent -20℃ 1 month;

Solubility

soluble in DMSO, HCl

In vitro: DMSO : 33.33 mg/mL 1 M HCl : 25 mg/mL

Documents

References

[1]. Yin L, et al. A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy. Eur J Med Chem. 2018 Jan 20;144:1-28.

Same target

Search CDK

Same research area

Search Cancer