D64131

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

D-64131 是一种微管蛋白聚合抑制剂，IC50 值为 0.53 μM。

D-64131 is a tubulin polymerization inhibitor with an IC50 value of 0.53 μM. The polymerization of bovine brain tubulin as well as binding of [3H] colchicine to biotinylated αβ-tubulin was dose-dependently inhibited by D-64131. Many Y cells display abnormal microtubule structures, such as fragmented mitotic spindles or multiple spindle poles after treatment with D-64131. Nuclear blebbing and abnormal nuclear structures typical for apoptotic cells are detectable in many cells treated with D-64131. In nude mice, D-64131 proved to be well tolerated and highly active against the human amelanoic melanoma MEXF 989 tumor xenograft. D-64131 treatment resulted in significant tumor growth inhibition during treatment.

D-64131 is antimitotic by binding to β-tubulin, thereby destabilizing microtubules and arresting mitotic cells in the M-phase.D-64131 inhibits the proliferation of tumor cells from 12 of 14 different organs and tissues with mean IC50s of 62 nM.D-64131 is cytotoxic toward MDR/MRP tumor cell lines.D-64131 suppresses U373 proliferation and cell cycle with IC50s of 74 nM and 62.7nM, respectively. Cell Cycle Analysis Cell Line:HeLa/KB cervical carcinoma cells Concentration:1 nM-1 μM Incubation Time:48 hours Result:Induced dose-dependently arrested in G2-M before induction of apoptotic cell death.

D-64131 (200-400 mg/kg; p.o.; daily; days 1-5, 8-9, and 15-18) significantly inhibits tumor growth in the human amelanoic melanoma MEXF 989 tumor xenograft mice model.D-64131 has oral bioavailability and is well tolerated at efficacious doses. Animal Model:Outbred nude mice (6-8 weeks),human amelanoic melanoma MEXF 989 tumor xenograft model Dosage:200 mg/kg, 400 mg/kg Administration:Oral administration, daily, on days 1-5, 8-9, and 15-18 after xenograft Result:Resulted in significant tumor growth inhibition during treatment.

D-64131 | D 64131 | D64131

Cytoskeleton/Cell Adhesion Molecules

Microtubule/Tubulin

Tubulin polymerization

Cancer

——

74588-78-6

251.28

C16H13NO2

>98% (HPLC)

Soluble in DMSO

O=C(C(N1)=CC2=C1C=CC(OC)=C2)C3=CC=CC=C3

(5-Methoxy-1H-indol-2-yl)phenylmeth?anone

(-20℃)

With Ice Pack

≥ 2 years