ODM-203 | CAS#1430723-35-5 | VEGFR Inhibitor

MedKoo Cat#: 206569 | Name: ODM-203

Description:

WARNING: This product is for research use only, not for human or veterinary use.

ODM-203 is an orally available inhibitor of the human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs), with potential antiangiogenic and antineoplastic activities. VEGFR/FGFR inhibitor ODM-203 inhibits both VEGFRs and FGFRs, which may result in the inhibition of VEGFR- and FGFR-mediated signaling. This leads to an inhibition of angiogenesis and cell proliferation in tumor cells overexpressing VEGFR and/or FGFR. Both VEGFRs and FGFRs belong to the superfamily of receptor tyrosine kinases and are upregulated in various tumor cell types.

Chemical Structure

ODM-203

CAS#1430723-35-5

Theoretical Analysis

MedKoo Cat#: 206569

Name: ODM-203

CAS#: 1430723-35-5

Chemical Formula: C26H21F2N5O2S

Exact Mass: 505.1384

Molecular Weight: 505.54

Elemental Analysis: Chemical Formula: C26H21F2N5O2S Exact Mass: 505.1384 Molecular Weight: 505.5438 Elemental Analysis: C, 61.77; H, 4.19; F, 7.52; N, 13.85; O, 6.33; S, 6.34

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,850.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 6,450.00	2 Weeks

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Synonym

ODM-203; ODM 203; ODM203

IUPAC/Chemical Name

N-(2',4'-Difluoro-5-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)-[1,1'-biphenyl]-3-yl)cyclopropanesulfonamide

InChi Key

ZJFCBQXPTQSTCZ-UHFFFAOYSA-N

InChi Code

InChI=1S/C26H21F2N5O2S/c1-32-14-18(13-30-32)16-2-7-26-25(10-16)29-15-33(26)21-9-17(23-6-3-19(27)11-24(23)28)8-20(12-21)31-36(34,35)22-4-5-22/h2-3,6-15,22,31H,4-5H2,1H3

SMILES Code

O=S(C1CC1)(NC2=CC(C3=CC=C(F)C=C3F)=CC(N4C=NC5=CC(C6=CN(C)N=C6)=CC=C45)=C2)=O

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

>2 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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC50 values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/2/1/4.

In vitro activity:

This report shows that ODM-203 inhibits FGFR and VEGFR family kinases selectively and with equal potency in the low nanomolar range (IC50 6-35 nmol/L) in biochemical assays. In cellular assays, ODM-203 inhibits VEGFR-induced tube formation (IC50 33 nmol/L) with similar potency as it inhibits proliferation in FGFR-dependent cell lines (IC50 50-150 nmol/L). Reference: Mol Cancer Ther. 2019 Jan;18(1):28-38. https://pubmed.ncbi.nlm.nih.gov/30301864/

In vivo activity:

In vivo, ODM-203 shows strong antitumor activity in both FGFR-dependent xenograft models and in an angiogenic xenograft model at similar well-tolerated doses. In addition, ODM-203 inhibits metastatic tumor growth in a highly angiogenesis-dependent kidney capsule syngenic model. Interestingly, potent antitumor activity in the subcutaneous syngenic model correlated well with immune modulation in the tumor microenvironment as indicated by marked decrease in the expression of immune check points PD-1 and PD-L1 on CD8 T cells and NK cells, and increased activation of CD8 T cells. Reference: Mol Cancer Ther. 2019 Jan;18(1):28-38. https://pubmed.ncbi.nlm.nih.gov/30301864/

	Solvent	mg/mL	mM
Solubility
	DMF	2.0	3.96
	DMSO	58.9	116.49
	DMSO:PBS (pH 7.2) (1:3)	0.3	0.49

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 505.54 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:

Holmström TH, Moilanen AM, Ikonen T, Björkman ML, Linnanen T, Wohlfahrt G, Karlsson S, Oksala R, Korjamo T, Samajdar S, Rajagopalan S, Chelur S, Narayanan K, Ramachandra RK, Mani J, Nair R, Gowda N, Anthony T, Dhodheri S, Mukherjee S, Ujjinamatada RK, Srinivas N, Ramachandra M, Kallio PJ. ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity. Mol Cancer Ther. 2019 Jan;18(1):28-38. doi: 10.1158/1535-7163.MCT-18-0204. Epub 2018 Oct 9. PMID: 30301864.

In vitro protocol:

In vivo protocol:

1: Holmström TH, Moilanen AM, Ikonen T, Björkman ML, Linnanen T, Wohlfahrt G, Karlsson S, Oksala R, Korjamo T, Samajdar S, Rajagopalan S, Chelur S, Narayanan K, Ramachandra RK, Mani J, Nair R, Gowda N, Anthony T, Dhodheri S, Mukherjee S, Ujjinamatada RK, Srinivas N, Ramachandra M, Kallio PJ. ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity. Mol Cancer Ther. 2019 Jan;18(1):28-38. doi: 10.1158/1535-7163.MCT-18-0204. Epub 2018 Oct 9. PubMed PMID: 30301864. 2: Bono P, Massard C, Peltola KJ, Azaro A, Italiano A, Kristeleit RS, Curigliano G, Lassen U, Arkenau HT, Hakulinen P, Garratt C, Ikonen T, Mustonen MVJ, Rodon JA. Phase I/IIa, open-label, multicentre study to evaluate the optimal dosing and safety of ODM-203 in patients with advanced or metastatic solid tumours. ESMO Open. 2020 Dec;5(6):e001081. doi: 10.1136/esmoopen-2020-001081. PMID: 33262202; PMCID: PMC7709506. 3: Ojala K, Salmia J, Shevchenko A, Ylikotila J, Korjamo T, van Veen B, Koistinen P, Malmström C, Laakso S, Bansal I, Samiulla DS, Juppo A. How to stop disproportionation of a hydrochloride salt of a very weakly basic compound in a non-clinical suspension formulation. Int J Pharm. 2021 Sep 5;606:120875. doi: 10.1016/j.ijpharm.2021.120875. Epub 2021 Jul 15. PMID: 34273425.