WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H405580
CAS#: 690206-97-4 (free base)
Description: ZM306416 is a selective VEGFR1 inhibitor. ZM306416 antagonizes the activity of KDR and Flt VEGF receptors with IC50 values of 100 nM and 2 μM, respectively.
Hodoodo Cat#: H405580
Name: ZM306416
CAS#: 690206-97-4 (free base)
Chemical Formula: C16H13ClFN3O2
Exact Mass: 333.07
Molecular Weight: 333.740
Elemental Analysis: C, 57.58; H, 3.93; Cl, 10.62; F, 5.69; N, 12.59; O, 9.59
Related CAS #: 196603-47-1 (HCl) 690206-97-4 (free base)
Synonym: ZM306416; ZM 306416; ZM-306416
IUPAC/Chemical Name: 4-[(4'-Chloro-2'-fluoro)phenylamino]-6,7-dimethoxyquinazoline
InChi Key: YHUIUSRCUKUUQA-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H13ClFN3O2/c1-22-14-6-10-13(7-15(14)23-2)19-8-20-16(10)21-12-4-3-9(17)5-11(12)18/h3-8H,1-2H3,(H,19,20,21)
SMILES Code: COC1=CC2=NC=NC(NC3=CC=C(Cl)C=C3F)=C2C=C1OC
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | ZM-306416 (CB 676475) is an inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. |
| In vitro activity: | The expression of primary alveolar osteoblast VEGF receptors and the subsequent effects on mineralization and nodule formation in vitro following VEGFR inhibition were investigated. The HAOBs (human alveolar osteoblasts) expressed high levels of VEGF and VEGFR1 protein but VEGFR2 was not detected. The VEGFR1/2 inhibitor, ZM306416, led to a dose-dependent decrease in mineralization. Reference: Aust Dent J. 2020 Sep;65(3):196-204. https://onlinelibrary.wiley.com/doi/10.1111/adj.12752 |
| In vivo activity: | TBD |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 55.7 | 166.81 | |
| DMF | 50.0 | 149.82 | |
| Ethanol | 20.0 | 59.93 |
The following data is based on the product molecular weight 333.74 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. McLaughlin KI, Milne TJ, Zafar S, Zanicotti DG, Cullinan MP, Seymour GJ, Coates DE. The in vitro effect of VEGF receptor inhibition on primary alveolar osteoblast nodule formation. Aust Dent J. 2020 Sep;65(3):196-204. doi: 10.1111/adj.12752. Epub 2020 Mar 27. PMID: 32072641. |
| In vitro protocol: | 1. McLaughlin KI, Milne TJ, Zafar S, Zanicotti DG, Cullinan MP, Seymour GJ, Coates DE. The in vitro effect of VEGF receptor inhibition on primary alveolar osteoblast nodule formation. Aust Dent J. 2020 Sep;65(3):196-204. doi: 10.1111/adj.12752. Epub 2020 Mar 27. PMID: 32072641. |
| In vivo protocol: | TBD |
1: McLaughlin KI, Milne TJ, Zafar S, Zanicotti DG, Cullinan MP, Seymour GJ, Coates DE. The in vitro effect of VEGF receptor inhibition on primary alveolar osteoblast nodule formation. Aust Dent J. 2020 Sep;65(3):196-204. doi: 10.1111/adj.12752. Epub 2020 Mar 27. PMID: 32072641.
2: Wu WB, Xu YY, Cheng WW, Yuan B, Zhao JR, Wang YL, Zhang HJ. Decreased PGF may contribute to trophoblast dysfunction in fetal growth restriction. Reproduction. 2017 Sep;154(3):319-329. doi: 10.1530/REP-17-0253. Epub 2017 Jul 4. PMID: 28676532.
3: Fujimoto T, Inoue T, Maki K, Inoue-Mochita M, Tanihara H. Vascular Endothelial Growth Factor-A Increases the Aqueous Humor Outflow Facility. PLoS One. 2016 Sep 1;11(9):e0161332. doi: 10.1371/journal.pone.0161332. PMID: 27584577; PMCID: PMC5008796.
4: Antczak C, Mahida JP, Bhinder B, Calder PA, Djaballah H. A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery. J Biomol Screen. 2012 Aug;17(7):885-99. doi: 10.1177/1087057112446174. Epub 2012 May 9. PMID: 22573732; PMCID: PMC3615554.
