Amuvatinib (MP-470)|2mg|K1295-上海高创化学科技有限公司

Amuvatinib (MP-470)

参考价：¥1298

供货周期：

7天

品牌：

型号：

2mg

货号：

K1295

SKU:K1295		M. Wt:447.51
Formula:C23H21N5O3S		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:850879-09-3		Synonyms:N/A
Chemical NameN/A

Description	Amuvatinib (MP-470)
Targets	c-Kit	PDGF-alpha	Flt3
IC50	10 nM	40 nM	81 nM
In vitro	MP470 exhibits low microM IC50 in prostate cancer cell lines. MP470 in combination with Erlotinib shows additive effects on both cytotoxicity and induction of apoptosis. MP470 reduced c-Met phosphorylation and enhanced radiation-induced cell kill by 0.4 logs in SF767 cells. MP470 was shown to inhibit dsDNA break repair and increase apoptosis. MP470 influences various survival and DNA repair related proteins such as pAKT, RAD51 and GSK3beta. Amuvatinib shows in vitro inhibitory activity against multiple human tyrosine kinases including mutant KIT and PDGFRalpha. Amuvaninib inhibited RAD51 protein expression and HR, which is associated with reduced ribosomal protein S6 phosphorylation and inhibition of global translation. Amuvatinib can sensitize cells to IR and MMC, agents that are selectively toxic to HR-deficient cells.
In vivo	In vivo, the addition of MP470 to radiation resulted in a tumor-growth-delay enhancement ratio of 2.9 over radiation alone and extended survival time. In human xenograft models in mice, amuvatinib is active as a DNA repair protein Rad51 inhibitor.The amuvatinib DPC formulation was well tolerated up to 1,500 mg/day. While exposures were low and variable, a transient response in a refractory GIST patient warrants further investigation into single-agent amuvatinib in refractory GIST. MP470 (Amuvatinib) can Downregulate and reverse EMT in mesenchymal normal human mammary epithelial cells and murine BCSCs attenuating self-renewal and restored chemosensitivity of the BCSCs.
Clinical Trials	N/A
Features	N/A

Description

Amuvatinib (MP-470)

Targets

c-Kit

PDGF-alpha

Flt3

IC50

10 nM

40 nM

81 nM

In vitro

MP470 exhibits low microM IC50 in prostate cancer cell lines. MP470 in combination with Erlotinib shows additive effects on both cytotoxicity and induction of apoptosis. MP470 reduced c-Met phosphorylation and enhanced radiation-induced cell kill by 0.4 logs in SF767 cells. MP470 was shown to inhibit dsDNA break repair and increase apoptosis. MP470 influences various survival and DNA repair related proteins such as pAKT, RAD51 and GSK3beta. Amuvatinib shows in vitro inhibitory activity against multiple human tyrosine kinases including mutant KIT and PDGFRalpha. Amuvaninib inhibited RAD51 protein expression and HR, which is associated with reduced ribosomal protein S6 phosphorylation and inhibition of global translation. Amuvatinib can sensitize cells to IR and MMC, agents that are selectively toxic to HR-deficient cells.

In vivo

In vivo, the addition of MP470 to radiation resulted in a tumor-growth-delay enhancement ratio of 2.9 over radiation alone and extended survival time. In human xenograft models in mice, amuvatinib is active as a DNA repair protein Rad51 inhibitor.The amuvatinib DPC formulation was well tolerated up to 1,500 mg/day. While exposures were low and variable, a transient response in a refractory GIST patient warrants further investigation into single-agent amuvatinib in refractory GIST. MP470 (Amuvatinib) can Downregulate and reverse EMT in mesenchymal normal human mammary epithelial cells and murine BCSCs attenuating self-renewal and restored chemosensitivity of the BCSCs.

Clinical Trials

N/A

Features

N/A