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BMS-777607

別名: BMS 817378

BMS-777607 (BMS 817378)是一種Met相關(guān)的抑制劑，作用于c-Met，Axl，Ron和Tyro3，在無細(xì)胞試驗(yàn)中IC50分別為3.9 nM，1.1 nM，1.8 nM和4.3 nM，作用于Met相關(guān)靶點(diǎn)比作用于Lck， VEGFR-2，和TrkA/B選擇性高40倍，比作用于其他受體和非受體激酶選擇性高500多倍。

BMS-777607 Chemical Structure

BMS-777607 Chemical Structure

CAS: 1025720-94-8

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 2041.38 現(xiàn)貨
5mg 976.53 現(xiàn)貨
50mg 5498.71 現(xiàn)貨
1g 16134.3 現(xiàn)貨
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BMS-777607相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

c-Met Signaling Pathways

c-Met信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
T-47D Function assay 10 μM Induces polyploidy by 86 % 23468529
ZR-75-1 Growth inhibitory assay ~5 μM inhibits cell proliferation 23468529
T-47D Growth inhibitory assay ~5 μM inhibits cell proliferation 23468529
KHT Growth inhibitory assay ~10 μM inhibits KHT cell proliferation 22286523
KHT Function assay ~0.5 μM inhibits cell invasion 22286523
KHT Function assay ~0.5 μM inhibits cell migration 22286523
KHT Function assay ~1 μM prevents spontaneous KHT cell scattering with IC50 of 0.1-0.5 μM 22286523
PC-3 Growth inhibitory assay ~10 μM reduces cell proliferation 20515943
DU145 Function assay 0.1 μM impairs HGF-mediated cell invasion 20515943
PC-3 Function assay 0.1 μM impairs HGF-mediated cell invasion 20515943
DU145 Function assay 0.01 μM suppresses HGF-induced cell migration 20515943
PC-3 Function assay 0.01 μM suppresses HGF-induced cell migration 20515943
DU145 Function assay 0.1 μM exhibits inhibitory effect on HGF-induced cell scattering 20515943
PC-3 Function assay 0.1 μM exhibits inhibitory effect on HGF-induced cell scattering 20515943
ZR-75-1 Function assay 10 μM Induces polyploidy by 88% 23468529
T-47D Function assay 10 μM inhibits AURK-B function and induces its protein degradation 23468529
CHRF Function assay 10 μM inhibits cell division 25304900
HPDE Function assay 10 μM blocks constitutive activation and decreased AKT signaling 26477314
U118MG Kinase assay ~3 μM blocks AXL phosphorylation 26848524
SF126 Kinase assay ~3 μM blocks AXL phosphorylation 26848524
U118MG Cytoxicity assay 12.5 μM decreases glioma cell viability 26848524
SF126 Cytoxicity assay 12.5 μM decreases glioma cell viability 26848524
U118MG Apoptosis assay 12.5 μM induces glioma cell apoptosis 26848524
SF126 Apoptosis assay 12.5 μM induces glioma cell apoptosis 26848524
U118MG Function assay 12.5 μM blocks glioma cell migration and invasive growth pattern 26848524
SF126 Function assay 12.5 μM blocks glioma cell migration and invasive growth pattern 26848524
GTL16 Function assay 6.25 mg/kg Cmax in human GTL16 cells xenografted athymic mouse at 6.25 mg/kg, po, Cmax = 4.5 μM. 19260711
GTL16 Function assay 50 mg/kg Cmax in human GTL16 cells xenografted athymic mouse at 50 mg/kg, po, Cmax = 43.7 μM. 19260711
GTL16 Function assay 30 mins Inhibition of Met phosphorylation in human GTL16 cells after 30 mins, IC50 = 0.02 μM. 19260711
GTL16 Antiproliferative assay 72 hrs Antiproliferative activity against Met-dependent human GTL16 cells after 72 hrs by MTS assay, IC50 = 0.1 μM. 19260711
NCI-H1993 Antiproliferative assay 72 hrs Antiproliferative activity against Met-dependent human NCI-H1993 cells after 72 hrs by MTS assay, IC50 = 0.15 μM. 19260711
U87 Antiproliferative assay 72 hrs Antiproliferative activity against Met-driven human U87 cells after 72 hrs by MTS assay, IC50 = 0.16 μM. 19260711
BAF3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BAF3 cells expressing TPR-Met assessed as growth inhibition after 72 hrs, IC50 = 0.1884 μM. 24792774
DU145 Antiinvasive assay 1 hr Antiinvasive activity in human DU145 cells assessed as inhibition of HGF-induced cell motility preincubated for 1 hr before HGF treatment measured after 24 hrs by cell scattering assay, IC50 = 0.2 μM. 24900830
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs, IC50 = 0.2858 μM. 24792774
NCI-H1993 Cytotoxicity assay 48 hrs Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay, IC50 = 1.108 μM. 24900830
MGHU3 Antiproliferative assay 72 hrs Antiproliferative activity against human MGHU3 cells after 72 hrs by CellTiter-Glo assay 30309671
RT112 Antiproliferative assay 72 hrs Antiproliferative activity against human RT112 cells after 72 hrs by CellTiter-Glo assay 30309671
KHT Kinase assay blocks the c-Met signaling pathway with IC50 of 10 nM 22286523
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
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生物活性

產(chǎn)品描述 BMS-777607 (BMS 817378)是一種Met相關(guān)的抑制劑，作用于c-Met，Axl，Ron和Tyro3，在無細(xì)胞試驗(yàn)中IC50分別為3.9 nM，1.1 nM，1.8 nM和4.3 nM，作用于Met相關(guān)靶點(diǎn)比作用于Lck， VEGFR-2，和TrkA/B選擇性高40倍，比作用于其他受體和非受體激酶選擇性高500多倍。
特性 BMS 777607是有效的Met家族成員抑制劑，比作用于Lck, VEGFR-2,和TrkA/B的選擇性高40多倍，比作用同樣其他受體和非受體激酶選擇性高500多倍。
靶點(diǎn)
Axl [1]
(Cell-free assay)		 RON [1]
(Cell-free assay)		 Met [1]
(Cell-free assay)		 Tyro3 [1]
(Cell-free assay)		 Mer [1]
(Cell-free assay)		 點(diǎn)擊更多
1.1 nM 1.8 nM 3.9 nM 4.3 nM 14 nM
體外研究(In Vitro)
體外研究活性

BMS-777607是ATP競(jìng)爭(zhēng)性Met激酶選擇性抑制劑，有效抑制c-Met自磷酸化，作用于GTL-16細(xì)胞裂解物， IC50為20 nM，且選擇性抑制Met驅(qū)動(dòng)的腫瘤細(xì)胞系如GTL-16細(xì)胞系, H1993和 U87增殖。[1] BMS-777607 作用于DU145前列腺癌細(xì)胞，抑制肝細(xì)胞生長(zhǎng)因子 (HGF)引起的c-Met自磷酸化， IC50<1 nM 。BMS 777607對(duì)腫瘤細(xì)胞生長(zhǎng)作用效果不大，但是作用于PC-3 和DU145 細(xì)胞，抑制HGF誘導(dǎo)的細(xì)胞分散。BMS 777607作用于這兩種細(xì)胞，也抑制刺激的細(xì)胞遷移和入侵，IC50<0.1 μM，這種作用存在劑量依賴性。[2] BMS 777607(~10 μM)作用于高度轉(zhuǎn)移性鼠科KHT細(xì)胞2小時(shí)，有效清除自磷酸化的c-Met水平，IC50為10 nM，不影響全部 c-Met,導(dǎo)致下游信號(hào)分子包括 ERK, Akt, p70S6K 和 S6受抑制，這種作用存在劑量依賴性。納摩爾級(jí)BMS-777607(~1 μM)處理24小時(shí),有效抑制KHT細(xì)胞分散，活動(dòng)，和入侵，這與MET基因抑制相關(guān),適當(dāng)影響細(xì)胞增殖和集落形成。[3]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 嚙齒類纖維肉瘤KHT細(xì)胞
濃度 溶于DMSO，作為儲(chǔ)存液(10 mM), 終濃度為10 μM 左右
孵育時(shí)間 2, 24和96小時(shí)
方法

用連續(xù)稀釋的BMS 777607 處理KHT細(xì)胞96小時(shí)，然后進(jìn)行MTT實(shí)驗(yàn)和臺(tái)酚藍(lán)排除，分別測(cè)定細(xì)胞增殖和細(xì)胞死亡。KHT細(xì)胞集落和BMS 777607溫育24小時(shí)，然后用結(jié)晶紫(0.1%)染色，然后顯影，測(cè)定細(xì)胞分散情況。使用無菌的1 ml吸管端在融合的KHT單層細(xì)胞上劃2 mm 痕，隨后用BMS-777607處理24小時(shí)，在4塊隨機(jī)區(qū)域中計(jì)數(shù)遷移到剝蝕地細(xì)胞數(shù)，用于測(cè)定細(xì)胞遷移情況。為了測(cè)定細(xì)胞入侵，用Matrigel預(yù)包被的轉(zhuǎn)移嵌入板(8 μm 孔膜)，和無血清培養(yǎng)基在有或無BMS 777607存在時(shí)，在37oC下溫育2小時(shí),使Matrigel再水化。懸浮在無血清培養(yǎng)基上的細(xì)胞裝到小室頂端，懸浮在含10% FBS的完全培養(yǎng)基上的細(xì)胞裝到小室底端，作為化學(xué)引誘物。溫育24小時(shí)，移除 Matrigel，用結(jié)晶紫染色。顯影并計(jì)數(shù)在濾液下面的入侵細(xì)胞。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot p-c-Met / c-Met / p-FAK / p-c-Src / p-Akt / p-S6K / p-S6 p53 / p21 / Survivin / p-Rb / Rb 22639908
Immunofluorescence α-tubulin / survivin 24444656
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

BMS 777607按6.25-50 mg/kg劑量口服處理給藥攜帶GTL-16人類移植瘤的無胸腺小鼠，明顯降低腫瘤體積，且沒有毒性。[1] BMS 777607按25 mg/kg劑量每天處理6-8周大的注射嚙齒類纖維肉瘤KHT細(xì)胞的雌性C3H/HeJ小鼠，降低 KHT肺腫瘤結(jié)節(jié)數(shù)量,提高形態(tài)出血, 且明顯修復(fù)損害轉(zhuǎn)移表型，與對(duì)照組相比，沒有明顯毒性。BMS 777607按 10 mg/kg 低劑量處理，也適度但不顯著抑制肺結(jié)節(jié)形成。[3]
動(dòng)物實(shí)驗(yàn) Animal Models 攜帶嚙齒類纖維肉瘤KHT細(xì)胞的雌性C3H/HeJ小鼠
Dosages 10-25 mg/kg
Administration 飼喂處理，每天一次
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01721148 Completed
Malignant Solid Tumour
ASLAN Pharmaceuticals
 October 2012 Phase 1
NCT00605618 Completed
Advanced Solid Tumors
Bristol-Myers Squibb
 March 2008 Phase 1|Phase 2

化學(xué)信息&溶解度

分子量 512.89 分子式

C25H19ClF2N4O4
CAS號(hào) 1025720-94-8 SDF Download BMS-777607 SDF
Smiles CCOC1=C(C(=O)N(C=C1)C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (194.97 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 1:
What formulation can we use to dissolve S1561 for mice in vivo study?

回答：
S1561 BMS-777607 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30 mg/ml is a suspension. It is fine for oral gavage. If you are going to use it for injection, please try the following vehicle: 4% DMSO+30% PEG 300+ddH2O. BMS-777607 can be dissolved in it at 5 mg/ml as a clear solution.

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