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5.30152

Cdc42/Rac1 Dual Inhibitor, AZA1

Synonym(s):

Cdc42/Rac1 Dual Inhibitor, AZA1, N²,N⁴- bis(2-Methyl-1H-indol-5-yl)pyrimidine-2,4-diamine, Cdc42 Inhibitor IV, Rac1 Inhibitor V

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Size/SKUAvailabilityPrice
10 mg
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$236.00

About This Item

Empirical Formula (Hill Notation):
C22H20N6
CAS Number:
Molecular Weight:
368.43
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
Assay:
≥95% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light

$236.00


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assay

≥95% (HPLC)

Quality Segment

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

light brown

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

SMILES string

CC1=CC2=C(N1)C=CC(=C2)NC3=NC(=NC=C3)NC4=CC5=C(C=C4)NC(=C5)C

InChI

1S/C22H20N6/c1-13-9-15-11-17(3-5-19(15)24-13)26-21-7-8-23-22(28-21)27-18-4-6-20-16(12-18)10-14(2)25-20/h3-12,24-25H,1-2H3,(H2,23,26,27,28)

InChI key

SYWHWWKOIJCMKF-UHFFFAOYSA-N

General description

A cell-permeable indolylpyrimidinediamine compound that selectively suppresses cellular levels of GTP-bound Rac1 and Cdc42, but not RhoA, in serum-starved prostate cancer cultures upon EGF-stimulation (% of non-stimulated control Rac1-GTP level with/without 20 µM AZA1 = 56/375 in 22Rv1, 30/235 in DU 154, and 12/118 in PC-3 cells; % of non-EGF-stimulated control Cdc42-GTP level with/without 20 µM AZA1 = 15/170 in 22Rv1, 30/105 in DU 154, and 12/100 in PC-3 cells), resulting in effective suppression of PAK1, Akt, and BAD phosphorylations, as well as time- and dose-dependent (2 to 10 µM and up to 72 hr) growth inhibition of the cells in serum-deprived cultures with or without EGF stimulation. Dual Cdc42/Rac1 inhibition by AZA1 also effectively inhibits prostate cancer cells migration by decreasing cellular F-/G-actin ratio and disabling both filopodia and lamepodia formation. Daily intraperitoneal injection (100 µg/100 µL 30% DMSO/mouse) is shown to be efficacious in suppressing 22Rv1 tumor expansion in mice in vivo.

Biochem/physiol Actions

Cell permeable: yes
Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Zins, K., et al. 2013. PLoS One8, e74924.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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This Item
500503509265500511
description

-

description

-

description

-

description

-

form

powder

form

solid

form

powder

form

oil

assay

≥95% (HPLC)

assay

≥94% (HPLC)

assay

≥97% (HPLC)

assay

≥97% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light


Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable



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