ZM306416
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MedKoo CAT#: 405580

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.


Chemical Structure

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ZM306416
CAS# 690206-97-4 (free base)

Theoretical Analysis

MedKoo Cat#: 405580
Name: ZM306416
CAS#: 690206-97-4 (free base)
Chemical Formula: C16H13ClFN3O2
Exact Mass: 333.06803
Molecular Weight: 333.74
Elemental Analysis: C, 57.58; H, 3.93; Cl, 10.62; F, 5.69; N, 12.59; O, 9.59

Price and Availability

Size Price Availability Quantity
25.0mg USD 90.0 Ready to ship
50.0mg USD 150.0 Ready to ship
100.0mg USD 250.0 Ready to ship
200.0mg USD 450.0 Ready to ship
500.0mg USD 950.0 Ready to ship
1.0g USD 1750.0 Ready to ship
2.0g USD 2950.0 Ready to ship
5.0g USD 5650.0 Ready to ship
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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

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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.67 166.81
DMF 50.0 149.82
Ethanol 20.0 59.93

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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

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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.



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