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ARRY334543
点击次数：332发布时间：2013/4/2 15:06:56
更新日期：2022/8/19 17:45:40
所 在 地：美洲
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详细内容
ARRY334543
上海义森生物科技有限公司
技术数据:
分子量（MW）: 466.94 
化学式: C22H19ClN6O2S
溶解度: DMSO 6mg/mL Water <1mg/mL Ethanol <1mg/mL 纯度: >99% 稳定性: at -20℃ CAS号: 845272-21-1, 1146629-86-8 （di4-methylbenzenesulfonate）
生物活性
ARRY334543 is a selective ａnd potent kinase ErbB-1 ａnd ErbB-2 inhibitor with IC50 of 7 ａnd 2 nM, respectively. [1] The Ki of ARRY334543 is 1 nM. ARRY334543 behaves as a reversible ATP-competitive inhibitor with nanomolar potency both in vitro ａnd in cell-based proliferation assays using A431 ａnd BT-474 cells. ARRY334543 is an AKT pathway inhibitor in cells that contains active ErbB-2 receptors. [1] ARRY334543 suppresses ErbB-2 ａnd ErbB-1 phosphorylation in human cancer cells, such as BT-474 with an IC50 of 43 nM ａnd A431 with an IC50 of 36 nM that overexpress ErbB-2 ａnd ErbB-1, respectively. [1] When dosed orally, ARRY334543 dose-dpendently inhibits growth of human tumor xenografts that overexpress ErbB-1 （A431） or ErbB-2 （MDA-MB-453）. ARRY334543 demonstrates significant dose related tumor growth prevention when administered orally, BID, for 21 days. [2] ARRY334543 has very good PK/ADME properties ａnd has revealed excellent activity in numerous mouse tumor xenograft models including epidermoid （A431）, breast （BT-474, MDA-MB-453）, non-small cell lung （H1650, A549, 292）, colorectal （Lovo, HT-29） ａnd gastric （N87） carcinoma models. In the BT-474 model, ARRY334543 demonstrates significant dose-related tumor growth inhibition by 69% at 100 mg/kg/d ａnd by 98% at 200 mg/kg/d. Excellent single agent activity for ARRY334543 in the SK-OV-3 ovarian carcinoma xenograft model as well as additive activity to trastuzumab in SK-OV-3, BT-474 ａnd NCI-N87 models has been demonstrated. ARRY334543 exhibits excellent additive activity ａnd tolerability with docetaxel. [2] ARRY334543 is carried out in a phase II clinical trial in the treatment of advanced cancer ａnd pancreatic cancer.
技术数据:
分子量（MW）: 466.94 化学式: C22H19ClN6O2S
溶解度: DMSO 6mg/mL Water <1mg/mL Ethanol <1mg/mL 纯度: >99% 稳定性: at -20℃ CAS号: 845272-21-1, 1146629-86-8 （di4-methylbenzenesulfonate）
生物活性
ARRY334543 is a selective ａnd potent kinase ErbB-1 ａnd ErbB-2 inhibitor with IC50 of 7 ａnd 2 nM, respectively. [1] The Ki of ARRY334543 is 1 nM. ARRY334543 behaves as a reversible ATP-competitive inhibitor with nanomolar potency both in vitro ａnd in cell-based proliferation assays using A431 ａnd BT-474 cells. ARRY334543 is an AKT pathway inhibitor in cells that contains active ErbB-2 receptors. [1] ARRY334543 suppresses ErbB-2 ａnd ErbB-1 phosphorylation in human cancer cells, such as BT-474 with an IC50 of 43 nM ａnd A431 with an IC50 of 36 nM that overexpress ErbB-2 ａnd ErbB-1, respectively. [1] When dosed orally, ARRY334543 dose-dpendently inhibits growth of human tumor xenografts that overexpress ErbB-1 （A431） or ErbB-2 （MDA-MB-453）. ARRY334543 demonstrates significant dose related tumor growth prevention when administered orally, BID, for 21 days. [2] ARRY334543 has very good PK/ADME properties ａnd has revealed excellent activity in numerous mouse tumor xenograft models including epidermoid （A431）, breast （BT-474, MDA-MB-453）, non-small cell lung （H1650, A549, 292）, colorectal （Lovo, HT-29） ａnd gastric （N87） carcinoma models. In the BT-474 model, ARRY334543 demonstrates significant dose-related tumor growth inhibition by 69% at 100 mg/kg/d ａnd by 98% at 200 mg/kg/d. Excellent single agent activity for ARRY334543 in the SK-OV-3 ovarian carcinoma xenograft model as well as additive activity to trastuzumab in SK-OV-3, BT-474 ａnd NCI-N87 models has been demonstrated. ARRY334543 exhibits excellent additive activity ａnd tolerability with docetaxel. [2] ARRY334543 is carried out in a phase II clinical trial in the treatment of advanced cancer ａnd pancreatic cancer.
技术数据:
分子量（MW）: 466.94 化学式: C22H19ClN6O2S
溶解度: DMSO 6mg/mL Water <1mg/mL Ethanol <1mg/mL 纯度: >99% 稳定性: at -20℃ CAS号: 845272-21-1, 1146629-86-8 （di4-methylbenzenesulfonate）
生物活性
ARRY334543 is a selective ａnd potent kinase ErbB-1 ａnd ErbB-2 inhibitor with IC50 of 7 ａnd 2 nM, respectively. [1] The Ki of ARRY334543 is 1 nM. ARRY334543 behaves as a reversible ATP-competitive inhibitor with nanomolar potency both in vitro ａnd in cell-based proliferation assays using A431 ａnd BT-474 cells. ARRY334543 is an AKT pathway inhibitor in cells that contains active ErbB-2 receptors. [1] ARRY334543 suppresses ErbB-2 ａnd ErbB-1 phosphorylation in human cancer cells, such as BT-474 with an IC50 of 43 nM ａnd A431 with an IC50 of 36 nM that overexpress ErbB-2 ａnd ErbB-1, respectively. [1] When dosed orally, ARRY334543 dose-dpendently inhibits growth of human tumor xenografts that overexpress ErbB-1 （A431） or ErbB-2 （MDA-MB-453）. ARRY334543 demonstrates significant dose related tumor growth prevention when administered orally, BID, for 21 days. [2] ARRY334543 has very good PK/ADME properties ａnd has revealed excellent activity in numerous mouse tumor xenograft models including epidermoid （A431）, breast （BT-474, MDA-MB-453）, non-small cell lung （H1650, A549, 292）, colorectal （Lovo, HT-29） ａnd gastric （N87） carcinoma models. In the BT-474 model, ARRY334543 demonstrates significant dose-related tumor growth inhibition by 69% at 100 mg/kg/d ａnd by 98% at 200 mg/kg/d. Excellent single agent activity for ARRY334543 in the SK-OV-3 ovarian carcinoma xenograft model as well as additive activity to trastuzumab in SK-OV-3, BT-474 ａnd NCI-N87 models has been demonstrated. ARRY334543 exhibits excellent additive activity ａnd tolerability with docetaxel. [2] ARRY334543 is carried out in a phase II clinical trial in the treatment of advanced cancer ａnd pancreatic cancer.
技术数据:
| 分子量（MW）: | 466.94 | |
|---|---|---|
| 化学式: | C22H19ClN6O2S | |
| 溶解度: | DMSO 6mg/mL Water <1mg/mL Ethanol <1mg/mL | |
| 纯度: | >99% | |
| 稳定性: | at -20℃ | |
| CAS号: | 845272-21-1, 1146629-86-8 （di4-methylbenzenesulfonate） |
生物活性
ARRY334543 is a selective ａnd potent kinase ErbB-1 ａnd ErbB-2 inhibitor with IC50 of 7 ａnd 2 nM, respectively. [1] The Ki of ARRY334543 is 1 nM. ARRY334543 behaves as a reversible ATP-competitive inhibitor with nanomolar potency both in vitro ａnd in cell-based proliferation assays using A431 ａnd BT-474 cells. ARRY334543 is an AKT pathway inhibitor in cells that contains active ErbB-2 receptors. [1] ARRY334543 suppresses ErbB-2 ａnd ErbB-1 phosphorylation in human cancer cells, such as BT-474 with an IC50 of 43 nM ａnd A431 with an IC50 of 36 nM that overexpress ErbB-2 ａnd ErbB-1, respectively. [1] When dosed orally, ARRY334543 dose-dpendently inhibits growth of human tumor xenografts that overexpress ErbB-1 （A431） or ErbB-2 （MDA-MB-453）. ARRY334543 demonstrates significant dose related tumor growth prevention when administered orally, BID, for 21 days. [2] ARRY334543 has very good PK/ADME properties ａnd has revealed excellent activity in numerous mouse tumor xenograft models including epidermoid （A431）, breast （BT-474, MDA-MB-453）, non-small cell lung （H1650, A549, 292）, colorectal （Lovo, HT-29） ａnd gastric （N87） carcinoma models. In the BT-474 model, ARRY334543 demonstrates significant dose-related tumor growth inhibition by 69% at 100 mg/kg/d ａnd by 98% at 200 mg/kg/d. Excellent single agent activity for ARRY334543 in the SK-OV-3 ovarian carcinoma xenograft model as well as additive activity to trastuzumab in SK-OV-3, BT-474 ａnd NCI-N87 models has been demonstrated. ARRY334543 exhibits excellent additive activity ａnd tolerability with docetaxel. [2] ARRY334543 is carried out in a phase II clinical trial in the treatment of advanced cancer ａnd pancreatic cancer.
