Fruquintinib
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MedKoo CAT#: 206175

CAS#: 1194506-26-7

Description: Fruquintinib, also known as HMPL-013, is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities. Upon oral administration, fruquintinib inhibits VEGF-induced phosphorylation of VEGFRs 1, 2, and 3 which may result in the inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and tumor cell death. Expression of VEGFRs may be upregulated in a variety of tumor cell types.


Chemical Structure

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Fruquintinib
CAS# 1194506-26-7

Theoretical Analysis

MedKoo Cat#: 206175
Name: Fruquintinib
CAS#: 1194506-26-7
Chemical Formula: C21H19N3O5
Exact Mass: 393.1325
Molecular Weight: 393.39
Elemental Analysis: C, 64.12; H, 4.87; N, 10.68; O, 20.34

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 Same day
25.0mg USD 250.0 Same day
50.0mg USD 450.0 Same day
100.0mg USD 750.0 Same day
200.0mg USD 950.0 Same day
500.0mg USD 1450.0 Same day
1.0g USD 2450.0 2 weeks
2.0g USD 4350.0 2 weeks
5.0g USD 6950.0 2 weeks
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Synonym: Fruquintinib; HMPL013; HMPL 013; HMPL-013.

IUPAC/Chemical Name: 6-((6,7-dimethoxyquinazolin-4-yl)oxy)-N,2-dimethylbenzofuran-3-carboxamide

InChi Key: BALLNEJQLSTPIO-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H19N3O5/c1-11-19(20(25)22-2)13-6-5-12(7-16(13)28-11)29-21-14-8-17(26-3)18(27-4)9-15(14)23-10-24-21/h5-10H,1-4H3,(H,22,25)

SMILES Code: O=C(C1=C(C)OC2=CC(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)=CC=C12)NC

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

Preparing Stock Solutions

The following data is based on the product molecular weight 393.39 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

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1: Sun Q, Zhou J, Zhang Z, Guo M, Liang J, Zhou F, Long J, Zhang W, Yin F, Cai H, Yang H, Zhang W, Gu Y, Ni L, Sai Y, Cui Y, Zhang M, Hong M, Sun J, Yang Z, Qing W, Su W, Ren Y. Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014 Sep 24:0. [Epub ahead of print] PubMed PMID: 25482937.

2: Gu Y, Wang J, Li K, Zhang L, Ren H, Guo L, Sai Y, Zhang W, Su W. Preclinical pharmacokinetics and disposition of a novel selective VEGFR inhibitor fruquintinib (HMPL-013) and the prediction of its human pharmacokinetics. Cancer Chemother Pharmacol. 2014 Jul;74(1):95-115. doi: 10.1007/s00280-014-2471-3. Epub 2014 May 11. PubMed PMID: 24817647.



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