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BMS-777607 (Synonyms: BMS-817378)

Catalog No.GC14214

BMS-777607 is a pan-TAM inhibitor, which shows anti-tumor activity to different types of cancer.

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BMS-777607 Chemical Structure

Cas No.: 1025720-94-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$62.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

CCA cell lines HuCCT1, KKU-100

Preparation Method

The HuCCT1 cells were cultured in RPMI-1640 medium. The KKU-100 cells were cultured in DMEM. All the cells were supplemented with 10% heat-inactivated FBS, 100 μg/ml streptomycin, 100 μg/ml penicillin, and 2 mM L glutamine in a humidified atmosphere containing 5% CO2 at 37˚C.

Reaction Conditions

Clonogenic assays were used to measure the growth of the HuCCT1 and KKU-100 cell lines, in the presence of varying concentrations of BMS 777607(1/3/5/10 μM).

Applications

BMS-777607 showed a concentration-dependent antiproliferative effect on both the HuCCT1 and KKU-100 cell lines. Moreover, in HuCCT1 and KKU-100 cell lines, IC50 values after treatment with BMS-777607 for 6 days were 11.4 and 5.9 μM, respectively. In addition, the expression of phospho-RON was decreased in both HuCCT1 and KKU-100 cell lines after treatment with BMS-777607.

Animal experiment [1]:

Animal models

adult male Sprague Dawley (SD) rats (310±14 g)

Preparation Method

The rats were administered 300 mg/l thioacetamide (TAA) via drinking water daily for up to 20 weeks. The gemcitabine/Oxaliplat -in treatment group received gemcitabine [50 mg/kg, intraperitoneal injection(i.p.)] and oxaliplatin (2 mg/kg, i.p.) once every 2 weeks over a 4-week period starting at the 21st week. The BMS-777607 treatment group received BMS-777607 [30 mg/kg, per os (p.o.)] 5 days/week starting at the 21st week. The control group rats received i.p. injections of PBS following the same schedule.

Dosage form

30 mg/kg, per os (p.o.)

Applications

BMS-777607 could significantly suppress the in vivo growth of CCA tumors in animal model.

References:

[1]. Cheng CT, et al. MET-RON dual inhibitor, BMS-777607, suppresses cholangiocarcinoma cell growth, and MET-RON upregulation indicates worse prognosis for intra-hepatic cholangiocarcinoma patients. Oncol Rep. 2018 Sep;40(3):1411-1421.

Background

BMS-777607 is a pan-TAM inhibitor, which shows anti-tumor activity to different types of cancer. BMS-777607 could also enhance the expression of proinflammatory cytokines and pro-immune cells over control with the combination anti-PD-1 treatment. The addition of BMS-777607 to anti- PD-1 treatment down-regulated immunosuppressive cytokines expression in tumor microenvironment. It has been reported that the combined treatment of BMS-777607 with anti-PD-1significantly decreased tumor growth and incidence of lung metastasis [1]

In vitro and in vivo experiment demonstrate that BMS-777607 could inhibit the growth of human CCA cells and decrease the expression of phospho-RON. Moreover, in HuCCT1 and KKU-100 cell lines, IC50 values after treatment with BMS-777607 for 6 days were 11.4 and 5.9 μM, respectively. BMS-777607 could also inhibit the in vivo growth of CCA in rats. [2]

References:
[1].Kasikara C, et al. Pan-TAM Tyrosine Kinase Inhibitor BMS-777607 Enhances Anti-PD-1 mAb Efficacy in a Murine Model of Triple-Negative Breast Cancer. Cancer Res. 2019 May 15;79(10):2669-2683.
[2].Cheng CT, et al. MET-RON dual inhibitor, BMS-777607, suppresses cholangiocarcinoma cell growth, and MET-RON upregulation indicates worse prognosis for intra-hepatic cholangiocarcinoma patients. Oncol Rep. 2018 Sep;40(3):1411-1421.

Chemical Properties

Cas No. 1025720-94-8 SDF
Synonyms BMS-817378
Chemical Name N-[4-(2-amino-3-chloropyridin-4-yl)oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide
Canonical 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
Formula C25H19ClF2N4O4 M.Wt 512.89
Solubility ≥ 25.65mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9497 mL 9.7487 mL 19.4974 mL
5 mM 0.3899 mL 1.9497 mL 3.8995 mL
10 mM 0.195 mL 0.9749 mL 1.9497 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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