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Chemical Structure| 1453208-66-6 Chemical Structure| 1453208-66-6
Chemical Structure| 1453208-66-6

ASP5878

CAS No.: 1453208-66-6

ASP5878 is an orally active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM, and 3.5 nM, respectively. ASP5878 has potential antitumor activity.

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Cat. No.: A494813 Purity: 99%

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Product Details of ASP5878

CAS No. :1453208-66-6
Formula : C18H19F2N5O4
M.W : 407.37
SMILES Code : COC1=CC(OC)=C(F)C(COC2=CN=C(NC3=CN(CCO)N=C3)N=C2)=C1F
MDL No. :MFCD30532771

Safety of ASP5878

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of ASP5878

RTK

Isoform Comparison

Biological Activity

Target
  • FGFR2

    FGFR2, IC50:0.6 nM

  • FGFR3

    FGFR3, IC50:0.74 nM

  • FGFR4

    FGFR4, IC50:3.5 nM

  • FGFR1

    FGFR1, IC50:0.47 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
G636C-FGFR4/3T3 cells 15.6 nM (IC50) 4 or 5 days To evaluate the antiproliferative effect of ASP5878 on G636C-FGFR4/3T3 cells, showing sensitivity to ASP5878. PMC6787178
G636C-FGFR4/BaF3 cells 34.4 nM (IC50) 4 or 5 days To evaluate the antiproliferative effect of ASP5878 on G636C-FGFR4/BaF3 cells, showing sensitivity to ASP5878 in the absence of IL-3. PMC6787178
ACH-iPSCs 10 nM from day 15 Increased the expression levels of chondrocytic markers ACAN and COL2A1, resulting in the formation of cartilaginous particles. PMC7708468

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Nude mice Subcutaneous xenograft model with G636C-FGFR4/3T3 cells Oral 3 mg/kg Once daily for 8 days To evaluate the antitumor activity of ASP5878 in a mouse xenograft model with G636C-FGFR4/3T3 cells, showing significant inhibition of tumor growth. PMC6787178
Mice Fgfr3Ach transgenic mice Subcutaneous injection 300 μg/kg Five times a week for 3 weeks Evaluated the effect of ASP5878 on bone growth in ACH model mice, showing that 300 μg/kg ASP5878 significantly elongated the femur and tibia lengths in male mice. PMC7708468

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02038673 Solid Tumors PHASE1 COMPLETED 2017-07-19 Site US402, Orange, California... More >>, 92868, United States|Site US401, New York, New York, 10032, United States|Site US404, Cleveland, Ohio, 44106, United States|Site US406, Spartanburg, South Carolina, 29303, United States|Site US410, Fairfax, Virginia, 22031, United States|Site US403, Seattle, Washington, 98109, United States|Site JP122, Chiba, Japan|Site JP108, Fukuoka, Japan|Site JP115, Fukuoka, Japan|Site JP120, Fukuoka, Japan|Site JP116, Hokkaido, Japan|Site JP113, Hyogo, Japan|Site JP103, Ibaraki, Japan|Site JP111, Ishikawa, Japan|Site JP119, Kanagawa, Japan|Site JP101, Kyoto, Japan|Site JP109, Miyagi, Japan|Site JP110, Miyagi, Japan|Site JP112, Nagoya, Japan|Site JP117, Niigata, Japan|Site JP121, Okayama, Japan|Site JP104, Osaka, Japan|Site JP106, Osaka, Japan|Site JP118, Osaka, Japan|Site JP124, Shizuoka, Japan|Site JP102, Tokyo, Japan|Site JP107, Tokyo, Japan|Site JP123, Tokyo, Japan|Site KR202, Gyeonggi-do, Korea, Republic of|Site KR201, Seoul, Korea, Republic of|Site KR203, Seoul, Korea, Republic of|Site KR204, Seoul, Korea, Republic of|Site TW302, Tainan, Taiwan|Site TW301, Taipei, Taiwan|Site TW303, Taipei, Taiwan Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.25mL

12.27mL

2.45mL

1.23mL

24.55mL

4.91mL

2.45mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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