ZM 306416

Catalog No.S2897 Batch:S289701

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Technical Data

Formula

C16H13ClFN3O2
Molecular Weight 333.74 CAS No. 690206-97-4
Solubility (25°C)* In vitro DMSO 67 mg/mL (200.75 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.
Targets
VEGFR1 [1] Src [1] Abl [1]
0.33 μM 0.33 μM 1.3 μM
In vitro ZM-306416 induces selective antiproliferative effect toward the EGFR-addicted NSCLC cell lines H3255 and HCC4011 with IC50 of 0.09 µM and 0.072 µM, respectively. ZM-306416 inhibits granule formation with IC50 of 0.67 μM. [1] ZM-306416 significantly inhibits the ERRα assay with IC50 of 7.3 μM in the GeneBLAzer T-Rex RORγ-UAS-bla HEK293T cell line. [2] ZM306416 (300 nM) completely inhibits PAA secretion and stimulates [125]I uptake in human thyroid follicular cells. ZM306416 (300 nM) abolishes pVEGFR2 (Y1214) expression in human thyroid follicular cells. ZM306416 (< 10 μM) has marked inhibitory effects on the steady state phosphorylation of p42/44 MAPK but does not affect the expression of the unphosphorylated form. ZM306416 (3 μM) significantly increases cell death in human thyroid follicular cells. ZM306416 (3 μM) significantly increases cell death in human thyroid follicular cells. ZM306416 weakly inhibits the secretion of VEGF and increases the production of PlGF. [3] ZM306416 (1 μM) enhances follicle formation and decreased nuclear distribution in human thyroid follicular cells. [4]

Protocol (from reference)

References

  • https://pubmed.ncbi.nlm.nih.gov/22573732/
  • https://pubmed.ncbi.nlm.nih.gov/21050030/
  • https://pubmed.ncbi.nlm.nih.gov/22227235/
  • https://pubmed.ncbi.nlm.nih.gov/21751212/

Customer Product Validation

<p>Panels D-F show morphological changes of RBEC cells due to Sema3A treatment. RBECs were fixed after the indicated treatment and stained with phalloidin conjugated with rhodamine (red color) and counter stained with DAPI (blue color). F-actin stress fibres are very clear in untreated cells (D). Sema3A treatment caused disruption of F-actin inside the cells. Densely packed bundles of cortical actin filaments started to appear along cell membranes (arrows) over the course of treatment with Sema3A. Antibodies and inhibitors against receptors of Sema3A were pre-incubated with the cells for 15 min before the addition of Sema3A. Antibodies to VEGFR1 and NRP2 (panel E) and the inhibitor Zm 306416 (selective to VEGFR1, panel F) were effective in ameliorating the effect of Sema3A. Scale bar=20 μm.</p>

, , Sci Rep, 2015, 5:7890.

<p>(B) Inhibitors of VEGFR prevent increase in p-Akt in cells bearing glycan-deficient PrP (panels 1 and 5). All cells were cultured in serum free medium and incubated with various chemical inhibitors. Cell lysates were prepared at the end of culture and immunoblotted with either anti-p-Akt (S473) or anti-Akt. Only inhibitors of VEGFR (panel 1) or VEGFR2 (panel 5) but not VEGFR1 (panel 3) or VEGFR3 (panel 7) diminish the levels of p-Akt in cells bearing glycan-deficient PrP.</p>

, , Cell Signal, 2016, 28(6):652-62.

SCE cells were treated with VEGF121 with or without ZM306416 (C) for 48 h. Data are expressed as the mean ± SD from eight (C) separate filters. *P < 0.05 and **P < 0.01 using the Tukey–Kramer HSD test.

Data from [ , , PLoS One, 2016, 11(9):e0161332 ]

Selleck's ZM 306416 Has Been Cited by 13 Publications

Gliovascular transcriptional perturbations in Alzheimer's disease reveal molecular mechanisms of blood brain barrier dysfunction [ Nat Commun, 2024, 15(1):4758] PubMed: 38902234
Regulation of Cell Cycle Progression through RB Phosphorylation by Nilotinib and AT-9283 in Human Melanoma A375P Cells [ Int J Mol Sci, 2024, 25(5)2956] PubMed: 38474202
Histamine promotes angiogenesis through a histamine H1 receptor-PKC-VEGF-mediated pathway in human endothelial cells [ J Pharmacol Sci, 2023, 151(4):177-186] PubMed: 36925216
Establishment of an oral squamous cell carcinoma cell line expressing vascular endothelial growth factor a and its two receptors [ J Dent Sci, 2022, 17(4):1471-1479] PubMed: 36299342
Vascular endothelial growth factor B exerts lipid-lowering effect by activating AMPK via VEGFR1 [ Life Sci, 2021, 276:119401] PubMed: 33785341
Crizotinib and Doxorubicin Cooperatively Reduces Drug Resistance by Mitigating MDR1 to Increase Hepatocellular Carcinoma Cells Death [ Front Oncol, 2021, 11:650052] PubMed: 34094940
The in vitro effect of VEGF receptor inhibition on primary alveolar osteoblast nodule formation. [ Aust Dent J, 2020, 10.1111/adj.12752] PubMed: 32072641
Central VEGF-A pathway plays a key role in the development of trigeminal neuropathic pain in rats. [ Mol Pain, 2019, 15:1744806919872602] PubMed: 31397622
Activated T cells induce proliferation of oligodendrocyte progenitor cells via release of vascular endothelial cell growth factor-A. [ Glia, 2018, 66(11):2503-2513] PubMed: 30500113
Vasculogenic and angiogenic potential of adipose stromal vascular fraction cell populations in vitro [Zakhari JS In Vitro Cell Dev Biol Anim, 2018, 54(1):32-40] PubMed: 29197029

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.