YO-01027 (Dibenzazepine),209984-56-5

Cat.No.:

IC-015654

Product Information

Biological Activity

YO-01027 (also called dibenzazepine; DBZ; YO01027) is a novel, potent, orally bioavailable, dipeptidic inhibitor of the ¦Ã-secretase with potential antineoplastic activity. It inhibits ¦Ã-secretase with IC50s of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively. It shows high in vivo antitumor efficacy in C57BL/6 mice bearing MCF-7 tumors.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species

Mouse

Rat

Rabbit

Guinea pig

Hamster

Dog

Weight (kg)

0.02

0.15

1.8

0.4

0.08

10

Body Surface Area (m2)

0.007

0.025

0.15

0.05

0.02

0.5

Km factor

3

6

12

8

5

20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by  (Animal B Km / Animal A Km)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Order Information

Quantity

Price($)

Price(€)

Availability

10mg

$160.00

€192.00

In stock

25mg

$260.00

€312.00

In stock

50mg

$420.00

€504.00

In stock

Free Delivery on orders over $350.00.

Chemical Information

Molecular Weight

463.48

Formula

C26H23F2N3O3

CAS Number

209984-56-5

Purity

>98.00%

Solubility

DMSO : 50 mg/mL (107.88 mM)

Storage

 -20¡æ

Reference

[1]. Groth C, et al. Pharmacological analysis of Drosophila melanogaster gamma-secretase with respect to differential proteolysis of Notch and APP. Mol Pharmacol. 2010 Apr;77(4):567-74.

[2]. Fuwa H, et al. Divergent synthesis of multifunctional molecular probes to elucidate the enzyme specificity of dipeptidic gamma-secretase inhibitors. ACS Chem Biol. 2007 Jun 15;2(6):408-18.

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