Linsitinib,867160-71-2

Cat.No.:IC-01249573

Product Information

Biological Activity

Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively[1].

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.

Chemical structure

Chemical Information

M.Weight

421.49

Formula

C26H23N5O

CAS No.

867160-71-2

Purity

 >98.00%

Solubility

50 mg/mL in DMSO

Storage

Keep in dark place,Sealed in
dry,Store in freezer, under -20¡ãC

Reference

1. Mulvihill MJ, et al. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and IR. Future Med Chem. 2009 Sep;1(6):1153-71.  [Content Brief]
2. McKinley ET, et al. 18FDG-PET predicts pharmacodynamic response to OSI-906, a dual IGF-1R/IR inhibitor, in preclinical mouse models of lung cancer. Clin Cancer Res. 2011 May 15;17(10):3332-40.  [Content Brief]
3. Li W, et al. Effectiveness of inhibitor rapamycin, saracatinib, linsitinib and JNJ-38877605 against human prostate cancer cells. Int J Clin Exp Med. 2015 Apr 15;8(4):6563-7.  [Content Brief]

Order Information

Cat./REF.

Size

Price($£©

Price(€)

Price(£¤/CNY£©

Price(£¤/JYP£©

IC-01249573

1ml(10mM)

$137.70

€ 165.24

£¤1,377.00

£¤27,402.30

IC-01249573

2mg

$92.20

€ 110.64

£¤922.00

£¤18,347.80

IC-01249573

5mg

$148.50

€ 178.20

£¤1,485.00

£¤29,551.50

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