PHA-767491|10mg|K1331-上海高创化学科技有限公司

PHA-767491

参考价：¥1056

供货周期：

一周

品牌：

规格：

10mg

货号：

K1331

CAS号：

845714-00-3

SKU:K1331		M. Wt:213.24
Formula:C12H11N3O		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:845714-00-3		Synonyms:N/A
Chemical NameN/A

Description	PHA-767491
Targets	Cdc7
IC50	0.6 nM(EC50)
In vitro	PHA-767491 is a potent Cdc7 inhibitor. PHA-767491 is the first molecule that directly affects the mechanisms controlling initiation as opposed to elongation in DNA replication. PHA-767491 blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites. PHA-767491 prevents the activation of replication origins but does not impede replication fork progression, and it does not trigger a sustained DNA damage response. PHA-767491 induced apoptosis in all CLL samples tested with an average EC50 of 0.6 uM. PHA-767491 activates the intrinsic apoptotic pathway in resting CLL cells. Exposure of CLL cells to 1 uM PHA-767491 induced Bax activation occurs upstream of caspase activation. PHA-767491 induces downregulation of Mcl-1 protein in a caspase-independent manner. And DNA synthesis and Cdc7 activity of IL-4 and CD154-stimulated CLL cells can be inhibited by PHA-767491.
In vivo	In preclinical cancer models, PHA-767491 shows inhibition to multiple cancer cell types and tumor growth.
Clinical Trials	N/A
Features	N/A

Description

PHA-767491

Targets

Cdc7

IC50

0.6 nM(EC50)

In vitro

PHA-767491 is a potent Cdc7 inhibitor. PHA-767491 is the first molecule that directly affects the mechanisms controlling initiation as opposed to elongation in DNA replication. PHA-767491 blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites. PHA-767491 prevents the activation of replication origins but does not impede replication fork progression, and it does not trigger a sustained DNA damage response. PHA-767491 induced apoptosis in all CLL samples tested with an average EC50 of 0.6 uM. PHA-767491 activates the intrinsic apoptotic pathway in resting CLL cells. Exposure of CLL cells to 1 uM PHA-767491 induced Bax activation occurs upstream of caspase activation. PHA-767491 induces downregulation of Mcl-1 protein in a caspase-independent manner. And DNA synthesis and Cdc7 activity of IL-4 and CD154-stimulated CLL cells can be inhibited by PHA-767491.

In vivo

In preclinical cancer models, PHA-767491 shows inhibition to multiple cancer cell types and tumor growth.

Clinical Trials

N/A

Features

N/A