製品番号: HY-12076

BMS 777607

(別名: BMS 817378)

12 Cited Publications

カスタマーレビュー

Based on 12 publication(s) in Google Scholar

BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC₅₀s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases.

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純度: 99.36%
CAS 番号: 1025720-94-8
分子式: C₂₅H₁₉ClF₂N₄O₄
分子量:512.89

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BMS 777607 構造式

CAS 番号: 1025720-94-8

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (12)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
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生物活性

製品説明

IC₅₀ & Target

Axl

Tyro3

TAM Receptor アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>10 μM Compound: BMS-777607	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 24900830]
ASPC1	GI₅₀	>10 μM Compound: 4; BMS-777607	Antiproliferative activity against human ASPC1 cells harbouring KRAS G12D mutant and RON delta 165 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human ASPC1 cells harbouring KRAS G12D mutant and RON delta 165 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
BaF3	IC₅₀	188.4 nM Compound: BMS-777607	Cytotoxicity against mouse BAF3 cells expressing TPR-Met assessed as growth inhibition after 72 hrs Cytotoxicity against mouse BAF3 cells expressing TPR-Met assessed as growth inhibition after 72 hrs	[PMID: 24792774]
CAPAN-1	GI₅₀	9.02 μM Compound: 4; BMS-777607	Antiproliferative activity against human CAPAN-1 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human CAPAN-1 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
DU-145	IC₅₀	200 nM Compound: BMS-777607	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 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	[PMID: 24900830]
EBC-1	IC₅₀	99.4 nM Compound: BMS-777607	Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay	[PMID: 27524312]
EBC-1	IC₅₀	162.3 nM Compound: BMS-777607	Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay	[PMID: 28412159]
GTL 16 cell line	IC₅₀	100 nM Compound: 10, BMS-777607	Antiproliferative activity against Met-dependent human GTL16 cells after 72 hrs by MTS assay Antiproliferative activity against Met-dependent human GTL16 cells after 72 hrs by MTS assay	[PMID: 19260711]
GTL 16 cell line	IC₅₀	100 nM Compound: 90; BMS-777607	Antiproliferative activity against human GTL 16 cell line assessed as inhibition of cell growth Antiproliferative activity against human GTL 16 cell line assessed as inhibition of cell growth	[PMID: 37262349]
HCC827	IC₅₀	>10 μM Compound: BMS-777607	Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay	[PMID: 24900830]
HCT-15	GI₅₀	5 μM Compound: 4; BMS-777607	Antiproliferative activity against human HCT-15 cells harbouring KRAS G13D mutant and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human HCT-15 cells harbouring KRAS G13D mutant and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
HepG2	IC₅₀	>1000 nM Compound: BMS-777607	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 28412159]
HT-29	GI₅₀	>10 μM Compound: 4; BMS-777607	Antiproliferative activity against human HT-29 cells harbouring wild-type KRAS and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human HT-29 cells harbouring wild-type KRAS and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
KM12C	GI₅₀	0.133 μM Compound: 4; BMS-777607	Antiproliferative activity against human KM12-C cells harbouring wild-type KRAS and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human KM12-C cells harbouring wild-type KRAS and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
LS-411N	GI₅₀	>10 μM Compound: 4; BMS-777607	Antiproliferative activity against human LS-411N cells harbouring wild-type KRAS and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human LS-411N cells harbouring wild-type KRAS and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
MIA PaCa-2	GI₅₀	>10 μM Compound: 4; BMS-777607	Antiproliferative activity against human MIA PaCa-2 cells harbouring KRAS G12C mutant and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human MIA PaCa-2 cells harbouring KRAS G12C mutant and RON delta 160 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
MKN-45	IC₅₀	285.8 nM Compound: BMS-777607	Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs	[PMID: 24792774]
NCI-H1975	IC₅₀	>10 μM Compound: BMS-777607	Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay	[PMID: 24900830]
NCI-H1993	IC₅₀	150 nM Compound: 10, BMS-777607	Antiproliferative activity against Met-dependent human NCI-H1993 cells after 72 hrs by MTS assay Antiproliferative activity against Met-dependent human NCI-H1993 cells after 72 hrs by MTS assay	[PMID: 19260711]
NCI-H1993	IC₅₀	1.108 μM Compound: BMS-777607	Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay	[PMID: 24900830]
NCI-H1993	IC₅₀	150 nM Compound: 90; BMS-777607	Antiproliferative activity against human NCI-H1993 cells assessed as inhibition of cell growth Antiproliferative activity against human NCI-H1993 cells assessed as inhibition of cell growth	[PMID: 37262349]
NCI-N87	IC₅₀	>10000 nM Compound: 10, BMS-777607	Antiproliferative activity against Met-independent human NCI-N87 cells after 72 hrs by MTS assay Antiproliferative activity against Met-independent human NCI-N87 cells after 72 hrs by MTS assay	[PMID: 19260711]
PANC-03-27	GI₅₀	>10 μM Compound: 4; BMS-777607	Antiproliferative activity against human Panc 03.27 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human Panc 03.27 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
PANC-1	GI₅₀	>10 μM Compound: 4; BMS-777607	Antiproliferative activity against human PANC-1 cells harbouring KRAS G12D mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human PANC-1 cells harbouring KRAS G12D mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
SW1417	GI₅₀	>10 μM Compound: 4; BMS-777607	Antiproliferative activity against human SW1417 cells harbouring wild-type KRAS and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human SW1417 cells harbouring wild-type KRAS and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
SW480	GI₅₀	>10 μM Compound: 4; BMS-777607	Antiproliferative activity against human SW480 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human SW480 cells harbouring KRAS G12V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
SW-620	GI₅₀	0.86 μM Compound: 4; BMS-777607	Antiproliferative activity against human SW620 cells harbouring KRAS G12 V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay Antiproliferative activity against human SW620 cells harbouring KRAS G12 V mutant and RON delta 155 assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 37736180]
T47D	IC₅₀	1417 nM Compound: BMS-777607	Effect on doxorubicin resistance in human T47D cells with compound-induced polyploidy assessed as change in doxorubicin-induced cytotoxicity by measuring increase in doxorubicin IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and sub Effect on doxorubicin resistance in human T47D cells with compound-induced polyploidy assessed as change in doxorubicin-induced cytotoxicity by measuring increase in doxorubicin IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and sub	[PMID: 23468529]
T47D	IC₅₀	2724 nM Compound: BMS-777607	Effect on bleomycin resistance in human T47D cells with compound-induced polyploidy assessed as change in bleomycin-induced cytotoxicity by measuring increase in bleomycin IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subsequen Effect on bleomycin resistance in human T47D cells with compound-induced polyploidy assessed as change in bleomycin-induced cytotoxicity by measuring increase in bleomycin IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subsequen	[PMID: 23468529]
T47D	IC₅₀	31.6 nM Compound: BMS-777607	Effect on paclitaxel resistance in human T47D cells with compound-induced polyploidy assessed as change in paclitaxel-induced cytotoxicity by measuring increase in paclitaxel IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subseq Effect on paclitaxel resistance in human T47D cells with compound-induced polyploidy assessed as change in paclitaxel-induced cytotoxicity by measuring increase in paclitaxel IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subseq	[PMID: 23468529]
T47D	IC₅₀	585 nM Compound: BMS-777607	Effect on methotrexate resistance in human T47D cells with compound-induced polyploidy assessed as change in methotrexate-induced cytotoxicity by measuring increase in methotrexate IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and Effect on methotrexate resistance in human T47D cells with compound-induced polyploidy assessed as change in methotrexate-induced cytotoxicity by measuring increase in methotrexate IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and	[PMID: 23468529]
T47D	IC₅₀	9.1 nM Compound: BMS-777607	Effect on cisplatin resistance in human T47D cells with compound-induced polyploidy assessed as change in cisplatin-induced cytotoxicity by measuring increase in cisplatin IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subsequen Effect on cisplatin resistance in human T47D cells with compound-induced polyploidy assessed as change in cisplatin-induced cytotoxicity by measuring increase in cisplatin IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subsequen	[PMID: 23468529]
U-87MG ATCC	IC₅₀	160 nM Compound: 10, BMS-777607	Antiproliferative activity against Met-driven human U87 cells after 72 hrs by MTS assay Antiproliferative activity against Met-driven human U87 cells after 72 hrs by MTS assay	[PMID: 19260711]
ZR-75-1	IC₅₀	1181 nM Compound: BMS-777607	Effect on doxorubicin resistance in human ZR-75-1 cells with compound-induced polyploidy assessed as change in doxorubicin-induced cytotoxicity by measuring increase in DOX IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subseque Effect on doxorubicin resistance in human ZR-75-1 cells with compound-induced polyploidy assessed as change in doxorubicin-induced cytotoxicity by measuring increase in DOX IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subseque	[PMID: 23468529]
ZR-75-1	IC₅₀	20.8 nM Compound: BMS-777607	Effect on paclitaxel resistance in human ZR-75-1 cells with compound-induced polyploidy assessed as change in paclitaxel-induced cytotoxicity by measuring increase in paclitaxel IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and sub Effect on paclitaxel resistance in human ZR-75-1 cells with compound-induced polyploidy assessed as change in paclitaxel-induced cytotoxicity by measuring increase in paclitaxel IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and sub	[PMID: 23468529]
ZR-75-1	IC₅₀	2263 nM Compound: BMS-777607	Effect on bleomycin resistance in human ZR-75-1 cells with compound-induced polyploidy assessed as change in bleomycin-induced cytotoxicity by measuring increase in bleomycin IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subseq Effect on bleomycin resistance in human ZR-75-1 cells with compound-induced polyploidy assessed as change in bleomycin-induced cytotoxicity by measuring increase in bleomycin IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subseq	[PMID: 23468529]
ZR-75-1	IC₅₀	3.4 nM Compound: BMS-777607	Effect on cisplatin resistance in human ZR-75-1 cells with compound-induced polyploidy assessed as change in cisplatin-induced cytotoxicity by measuring increase in cisplatin IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subseq Effect on cisplatin resistance in human ZR-75-1 cells with compound-induced polyploidy assessed as change in cisplatin-induced cytotoxicity by measuring increase in cisplatin IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout and subseq	[PMID: 23468529]
ZR-75-1	IC₅₀	430 nM Compound: BMS-777607	Effect on methotrexate resistance in human ZR-75-1 cells with compound-induced polyploidy assessed as change in methotrexate-induced cytotoxicity by measuring increase in methotrexate IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout a Effect on methotrexate resistance in human ZR-75-1 cells with compound-induced polyploidy assessed as change in methotrexate-induced cytotoxicity by measuring increase in methotrexate IC50 at 5 umol/L preincubated for 72 hrs followed by compound washout a	[PMID: 23468529]

体外実験

BMS 777607 is a selective ATP-competitive Met kinase inhibitor which potently blocks the autophosphorylation of c-Met with IC₅₀ of 20 nM in GTL-16 cell lysates, and demonstrates selective inhibition of proliferation in Met-driven tumor cell lines, such as GTL-16 cell line, H1993 and U87^[1]. BMS 777607 inhibits hepatocyte growth factor (HGF)-triggered c-Met autophosphorylation with IC₅₀ of < 1 nM in PC-3 and DU145 prostate cancer cells. BMS 777607 has little effect on tumor cell growth, but exhibits inhibitory effect on HGF-induced cell scattering in PC-3 and DU145 cells, with almost complete inhibition at 0.5 μM. BMS 777607 also suppresses stimulated cell migration and invasion in a dose-dependent fashion (IC₅₀ < 0.1 μM) in both cell lines^[2]. Application of BMS 777607 (appr 10 μM) to the highly metastatic murine KHT cells for 2 hours potently eliminates basal levels of autophosphorylated c-Met with IC₅₀ of 10 nM without affecting the total c-Met, leading to dose-dependent inhibition of phosphorylation of downstream signaling molecules including ERK, Akt, p70S6K and S6. Treatment with BMS 777607 (appr 1 μM) for 24 hours potently inhibits the KHT cell scatter, motility and invasion at doses in the nanomolar range which consists with MET gene knockdown, and modestly affects cell proliferation and colony formation^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Oral administration of BMS 777607 (6.25-50 mg/kg) significantly reduces tumor volumes of the GTL-16 human tumor xenografts in athymic mice with no observed toxicity^[1]. Administration of BMS 777607 (25 mg/kg/day) decreases the number of KHT lung tumor nodules (28.3%), improves the morphological hemorrhage, and significantly impairs the metastatic phenotype in the 6-8 week-old female C3H/HeJ mice injected with rodent fibrosarcoma KHT cells without apparent systemic toxicity compared to the control treatment. A low dose of BMS 777607 (10 mg/kg) also offers a mild but not significant inhibition of lung nodule formation compared to the vehicle control^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1025720-94-8
性状 Solid
分子量 512.89
分子式 C₂₅H₁₉ClF₂N₄O₄
Color White to off-white
SMILES

O=C(NC1=CC=C(C(F)=C1)OC2=C(C(N)=NC=C2)Cl)C3=C(C=CN(C3=O)C4=CC=C(C=C4)F)OCC
別名

BMS 817378
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

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Journal Impact Factor

ACS Nano

Efferocytosis Nanoinhibitors to Promote Secondary Necrosis and Potentiate the Immunogenicity of Conventional Cancer Therapies for Improved Therapeutic Benefits. [Abstract]

2023 Sep 26;17(18):18089-18102. PMID: 37669546
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Acta Pharmacol Sin

Circulating small extracellular vesicles promote proliferation and migration of vascular smooth muscle cells via AXL and MerTK activation. [Abstract]

2023 May;44(5):984-998. PMID: 36450791
Biochem Pharmacol

Phosphatidylserine-Rich circulating extracellular vesicles activate TAM receptor signaling to promote skin wound repair. [Abstract]

2026 Jul:249:117941. PMID: 41921755
Biochem Pharmacol

Cabozantinib inhibits necroptosis by targeting MLKL oligomerization and alleviates psoriasis in vivo. [Abstract]

2026 Jun:248:117843. PMID: 41747872
Cells

Loss of MER Tyrosine Kinase Attenuates Adipocyte Hypertrophy and Leads to Enhanced Thermogenesis in Mice Exposed to High-Fat Diet. [Abstract]

2024 Nov 18;13(22):1902. PMID: 39594650
Liver Int

The MSP-RON pathway regulates liver fibrosis through transforming growth factor beta-dependent epithelial-mesenchymal transition. [Abstract]

2021 Aug;41(8):1956-1968. PMID: 33786995
Cancer Res Treat

RON and MET Co-overexpression Are Significant Pathological Characteristics of Poor Survival and Therapeutic Targets of Tyrosine Kinase Inhibitors in Triple-Negative Breast Cancer. [Abstract]

2020 Jul;52(3):973-986. PMID: 32324988
Exp Cell Res

A C-Met chemical inhibitor promotes fracture healing through interacting with osteogenic differentiation via the mTORC1 pathway. [Abstract]

2019 Aug 1;381(1):50-56. PMID: 31034806

BMS 777607 purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2019 Aug 1;381(1):50-56. [Abstract]

Western analysis of the effect of BMS-777607 on the expression of osteogenic biomarkers during the osteoblastic differentiation of cultured preosteoblastic cells for 4 days.
World J Gastrointest Oncol

Pathological significance of abnormal recepteur d'origine nantais and programmed death ligand 1 expression in colorectal cancer. [Abstract]

2020 Nov 15;12(11):1216-1236. PMID: 33250957
Taiwan J Obstet Gynecol

Antitumor effects of BMS-777607 on ovarian cancer cells with constitutively activated c-MET. [Abstract]

2019 Jan;58(1):145-152. PMID: 30638469

BMS 777607 purchased from MedChemExpress. Usage Cited in: Taiwan J Obstet Gynecol. 2019 Jan;58(1):145-152. [Abstract]

Western blot of c-MET signaling-associated proteins of the SKOV3 cells treated with BMS-777607.

BMS 777607 purchased from MedChemExpress. Usage Cited in: Taiwan J Obstet Gynecol. 2019 Jan;58(1):145-152. [Abstract]

Western blot of cell cycle- and mitosis-associated proteins in SKOV3 cells treated with BMS-777607 for 48 h.
Research Square Preprint

2020 Jun.

溶剤 & 溶解度

体外:

DMSO : 83.33 mg/mL (162.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9497 mL

9.7487 mL

19.4974 mL

5 mM

0.3899 mL

1.9497 mL

3.8995 mL

10 mM

0.1950 mL

0.9749 mL

1.9497 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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Mass Mass

濃度濃度

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分子量分子量

希釈計算機

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濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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Please enter the basic information of animal experiments:

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Please enter your animal formula composition:

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

Cell Assay^[3]

KHT cells are exposed to serial dilution of BMS 777607 for 96 hours, then the MTT assay and trypan blue exclusion are used for the determination of cell proliferation and cell death, respectively. KHT cell colonies are incubated with BMS 777607 for 24 hours and then stained with crystal violet (0.1%) and photographed for the assessment of cell scattering. 2 mm scratch on the confluent KHT cell monolayer is made using a sterilized 1 mL pipette tip followed by treated with BMS 777607 for 24 hours, then the number of cells that have migrated into the denuded area is counted on 4 random fields for the evaluation of cell migration. For the examination of cell invasion, the commercial transwell inserts (8 μM pore membrane) pre-loaded with Matrigel are incubated with serum-free medium in the presence or absence of BMS 777607 at 37°C for 2 hours to allow rehydration of Matrigel. Then cells suspended in serum-free medium are loaded onto the top chamber (5×10³/insert) and complete medium (containing 10% FBS) is used in the lower chamber as a chemoattractant. After incubation for 24 hours, the Matrigel is removed and the inserts are stained with crystal violet. Invaded cells on the underside of the filter are photographed and counted.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

The pharemacokinetics of BMS 777607 are characterized in male Balb/C mice. Two groups of animals (N=6 per group, 20-25 g) are fasted overnight and receive BMS 777607 either as an intravenous (IV) bolus dose (5 mg/kg) via the tail vein or by gavage (10 mg/kg). The mice are fed 6 h after dosing. Blood samples (appr 0.2 mL) are obtained by retro-orbital bleeding at 0.05 (or 0.25 for oral), 0.5, 1, 3, 6, 8 and 24 h post dose. Within each group, half of the animals are bled at 0.05 (or 0.25 for oral), 1, 6 and 24 h, the other half are bled at 0.5, 3, and 8 h, resulting in a composite pharmacokinetic profile (3 mice per time point). Blood samples are allowed to coagulate and centrifuged at 4°C (1500-2000 ×g) to obtain serum. Serum samples are stored at appr 20°C until analysis by LC/MS/MS.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Schroeder GM, et al. Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily. J Med Chem. 2009 Mar 12;52(5):1251-4. [Content Brief]

[2]. Dai Y, et al. BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. Mol Cancer Ther, 2010, 9(6), 1554-1561. [Content Brief]

[3]. Dai Y, et al. Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation. Clin Exp Metastasis, 2012, 29, 253-261. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9497 mL	9.7487 mL	19.4974 mL	48.7434 mL
	5 mM	0.3899 mL	1.9497 mL	3.8995 mL	9.7487 mL
	10 mM	0.1950 mL	0.9749 mL	1.9497 mL	4.8743 mL
	15 mM	0.1300 mL	0.6499 mL	1.2998 mL	3.2496 mL
	20 mM	0.0975 mL	0.4874 mL	0.9749 mL	2.4372 mL
	25 mM	0.0780 mL	0.3899 mL	0.7799 mL	1.9497 mL
	30 mM	0.0650 mL	0.3250 mL	0.6499 mL	1.6248 mL
	40 mM	0.0487 mL	0.2437 mL	0.4874 mL	1.2186 mL
	50 mM	0.0390 mL	0.1950 mL	0.3899 mL	0.9749 mL
	60 mM	0.0325 mL	0.1625 mL	0.3250 mL	0.8124 mL
	80 mM	0.0244 mL	0.1219 mL	0.2437 mL	0.6093 mL
	100 mM	0.0195 mL	0.0975 mL	0.1950 mL	0.4874 mL

Keywords

BMS 777607

12 Cited Publications

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BMS 777607

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MedChemExpress（MCE）の使用を引用している文献 BMS 777607

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Publications (12)

溶剤 & 溶解度

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純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

BMS 777607 関連分類

製品番号: HY-12076