1. Protein Tyrosine Kinase/RTK
  2. FGFR
    VEGFR
  3. ACTB-1003

ACTB-1003 

Cat. No.: HY-16025 Purity: 97.65%
Handling Instructions

ACTB-1003 is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.

For research use only. We do not sell to patients.

ACTB-1003 Chemical Structure

ACTB-1003 Chemical Structure

CAS No. : 939805-30-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 328 In-stock
Estimated Time of Arrival: December 31
2 mg USD 168 In-stock
Estimated Time of Arrival: December 31
5 mg USD 252 In-stock
Estimated Time of Arrival: December 31
10 mg USD 420 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

ACTB-1003 is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.

IC50 & Target

FGFR1

6 nM (IC50)

VEGFR2

2 nM (IC50)

Tie-2

4 nM (IC50)

In Vitro

ACTB-1003 is an oral kinase inhibitor with multiple modes of action, targeting cancer mutations via FGFR inhibition FGFR1 (IC50=6 nM), angiogenesis through inhibition of VEGFR2 (2 nM), Tie-2 (4 nM), and induces apoptosis likely by targeting RSK (5 nM) and p70S6K (32 nM). ACTB-1003 is highly active with dose-dependent tumor growth inhibition in cell lines with FGFR genetic alterations - OPM2 human multiple myeloma and the murine leukemia Ba/F3-TEL-FGFR1. OPM2 cells harbor the FGFR3 t(4:14) translocation, FGFR3 K650E mutation and PTEN deletion while the Ba/F3-TEL-FGFR1 cells are driven by FGFR1 over-expression[1].

In Vivo

ACTB-1003 is shown to inhibit tumor angiogenesis evident by the inhibition of CD31 staining in tumor sections. ACTB-1003 is combinable with 5-FU or paclitaxel without diminishing the activity or increasing the toxicity of these chemotherapy agents in the HCT-116 colon tumor xenograft model[1].

Molecular Weight

591.53

Formula

C₂₇H₂₆F₅N₇O₃

CAS No.

939805-30-8

SMILES

O=C(NC1=CC(C(F)(F)F)=CC=C1F)NC2=CC=C(C3=C4C(N)=NC=NN4C(CN5CCOCC5)=C3COC)C=C2F

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (59.17 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6905 mL 8.4527 mL 16.9053 mL
5 mM 0.3381 mL 1.6905 mL 3.3811 mL
10 mM 0.1691 mL 0.8453 mL 1.6905 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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ACTB-1003
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HY-16025
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