135897-06-2

Synonym(s):
9,10,11,12,-Tetrahydro-9,12-epoxy-1 H-diindolo(1,2,3-fg:3ʹ,2ʹ,1ʹ-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-1,3(2 H)-dione, Chk1 Inhibitor I;9,10,11,12,-Tetrahydro-9,12-epoxy-1H-diindolo(1,2,3-fg:3ʹ,2ʹ,1ʹ-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-1,3(2H)-dione, Chk1 Inhibitor I;SB 218078 - CAS 135897-06-2 - Calbiochem

CAS NO.：135897-06-2

Empirical Formula: C24H15N3O3

Molecular Weight: 393.39

MDL number:

PRODUCT Properties

• Melting point: >340 °C
• Density: 1.80±0.1 g/cm3(Predicted)
• storage temp.: Store at RT
• solubility: ≤5mg/ml in DMSO;5mg/ml in dimethyl formamide
• form: crystalline solid
• pka: 9.75±0.20(Predicted)
• color: Light yellow to yellow
• InChI: 1S/C24H15N3O3/c28-23-19-17-11-5-1-3-7-13(11)26-15-9-10-16(30-15)27-14-8-4-2-6-12(14)18(22(27)21(17)26)20(19)24(29)25-23/h1-8,15-16H,9-10H2,(H,25,28,29)
• InChIKey: OTPNDVKVEAIXTI-UHFFFAOYSA-N

Description and Uses

SB 218078 is an inhibitor of checkpoint kinase 1 (Chk1) that blocks phosphorylation of cdc25 with an IC₅₀ value of 15 nM. It less potently inhibits cdc2 and PKC (IC₅₀s = 250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 μM. SB 218078 releases G₂ cell cycle arrest induced by γ-irradiation or the topoisomerase I inhibitor topotecan . In this way, SB 218078 enhances the cytotoxicity of DNA-damaging compounds.

SB 218078 is a selective inhibitor of Chk1.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302-H315-H319-H335
• Precautionary statements: P261-P305+P351+P338
• WGK Germany: WGK 1
• Storage Class: 11 - Combustible Solids