1. Protein Tyrosine Kinase/RTK
  2. VEGFR

Fruquintinib (Synonyms: HMPL-013)

Cat. No.: HY-19912 Purity: 99.93%
Data Sheet SDS Handling Instructions

Fruquintinib (HMPL-013) inhibits VEGFR family member (VEGFR1, 2, 3) with IC50s of 33 nM, 35 nM and 0.5 nM, respectively with weak inhibition of RET, FGFR-1 and c-kit kinases.

For research use only. We do not sell to patients.
Fruquintinib Chemical Structure

Fruquintinib Chemical Structure

CAS No. : 1194506-26-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO $110 In-stock
5 mg $100 In-stock
10 mg $150 In-stock
50 mg $450 In-stock
100 mg $750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Fruquintinib (HMPL-013) inhibits VEGFR family member (VEGFR1, 2, 3) with IC50s of 33 nM, 35 nM and 0.5 nM, respectively with weak inhibition of RET, FGFR-1 and c-kit kinases. IC50 value: 33/35/ 0.5 nM (VEGFR1/2/3) Target: VEGFR in vitro: Fruquintinib (HMPL-013) is a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Fruquintinib inhibits VEGFR2 (KDR) with an IC50 of 25 nM in the Z-lyte assay. Fruquintinib suppresses VEGF/VEGFR signaling and cell proliferation in HUVECs and HLECs. Fruquintinib inhibits tubule sprouting and prevents angiogenesis. [1] in vivo: Fruquintinib potently inhibits VEGF induced KDR phosphorylation in lung tissue of mouse. Fruquintinib inhibits tumor growth in multiple human xenograft models. [1]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01955304 Hutchison Medipharma Limited Food Effect of Fruquintinib in Health Subjects June 2012 Phase 1
NCT02689752 Hutchison Medipharma Limited Healthy July 2016 Phase 1
NCT02415023 Hutchison Medipharma Limited Gastric Cancer September 2014 Phase 1|Phase 2
NCT01645215 Hutchison Medipharma Limited|Fudan University Tumor January 2011 Phase 1
NCT01975077 Hutchison Medipharma Limited|Fudan University|Sun Yat-sen University Colorectal Cancer December 2012 Phase 1|Phase 2
NCT02976116 Hutchison Medipharma Limited NSCLC December 2016 Phase 2
NCT02314819 Hutchison Medipharma Limited|Fudan University|Eighty-One Hospital of People's Liberation Army Colorectal Cancer December 2014 Phase 3
NCT02196688 Hutchison Medipharma Limited|Fudan University|Sun Yat-sen University Colorectal Cancer April 2014 Phase 2
NCT02691299 Hutchison Medipharma Limited NSCLC September 2015 Phase 3
NCT02590965 Hutchison Medipharma Limited|Shanghai Chest Hospital Non-small Cell Lung Cancer April 2014 Phase 2
NCT03223376 Hutchison Medipharma Limited|Sun Yat-sen University Advanced Gastric Cancer September 2017 Phase 3
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.5420 mL 12.7100 mL 25.4201 mL
5 mM 0.5084 mL 2.5420 mL 5.0840 mL
10 mM 0.2542 mL 1.2710 mL 2.5420 mL
References
Molecular Weight

393.39

Formula

C₂₁H₁₉N₃O₅

CAS No.

1194506-26-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 7.75 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.93%

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Product Name:
Fruquintinib
Cat. No.:
HY-19912
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