[CAS NO. 436133-68-5] Kobe0065

Name: Kobe0065
Brand: Arctom Scientific
SKU: SLK-S8303

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PRODUCTS SPECIFICATIONS [436133-68-5]

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Catalog

SLK-S8303

Brand

Selleck

CAS

436133-68-5

DESCRIPTION [436133-68-5]

Overview

MDL	-
Molecular Weight	449.79
Molecular Formula	C15H11ClF3N5O4S
SMILES	-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.2233 mL	11.1163 mL	22.2326 mL
5 mM	0.4447 mL	2.2233 mL	4.4465 mL
10 mM	0.2223 mL	1.1116 mL	2.2233 mL
50 mM	0.0445 mL	0.2223 mL	0.4447 mL

Description

Kobe0065 is interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.

Targets

H-Ras-cRaf1 interaction ^[1]

In vitro

Kobe0065-family compounds bind to Ras⋅GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras⋅GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition.

In vivo

Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss.

References

[1] Shima F, et al. Proc Natl Acad Sci U S A. 2013, 110(20):8182-7.