| Cas No.: | 891494-63-6 |
| Chemical Name: | SCH-900776; SCH 900776, MK-8776. |
| Synonyms: | SCH-900776; SCH 900776, MK-8776. |
| SMILES: | C12=C(C3=CN(C)N=C3)C=NN1C(N)=C(Br)C([C@H]1CCCNC1)=N2 |
| Formula: | C15H18BrN7 |
| M.Wt: | 376.25 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | SCH900776 is a potent, selective and oral inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. It shows 50- and 500-fold selectivity over CDK2 andChk2, respectively. |
| In Vivo: | SCH 900776 induces the γ-H2AX biomarker at 4 mg/kg (i.p.), and enhances tumor pharmacodynamic and regression responses in A2780 xenograft model. SCH 900776 (16 and 32 mg/kg, i.p.) induces incremental improvements in tumor response. Escalation of SCH 900776 dose to 20 and 50 mg/kg in combination with gemcitabine results in improvements in TTP 10× in the A2780 xenograft systems[2]. |
| In Vitro: | SCH900776 (300 nM) shows potent inhibitory activities against phosphorylation at ser296-Chk1. SCH900776 (1 μM) causes a 30-fold decrease in the IC50 for hydroxyurea in MDA-MB-231 cells[1]. The Kd value of SCH 900776 for the CHK1 kinase domain is 2 nM. SCH 900776 exhibits an approximate EC50 of 60 nM in cells exposure to hydroxyurea. SCH 900776 induces dose-dependent suppression of CHK1 pS296 and concomitant accumulation of phospho-RPA signal in U2OS cells[2]. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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