1. Protein Tyrosine Kinase/RTK
  2. FGFR

CH5183284 (Synonyms: Debio 1347)

Cat. No.: HY-19957 Purity: 99.17%
Data Sheet SDS Handling Instructions

CH5183284 is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

For research use only. We do not sell to patients.
CH5183284 Chemical Structure

CH5183284 Chemical Structure

CAS No. : 1265229-25-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $190 In-stock
25 mg $330 In-stock
50 mg $500 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

CH5183284 is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

IC50 & Target

IC50: 9.3 nM (FGFR1), 7.6 nM (FGFR2), 22 nM (FGFR3), 290 nM (FGFR4)[1]

In Vitro

CH5183284 is well balanced in cellular antiproliferative activity against SNU-16 and stability in human liver microsome. The selectivity of 8 to inhibit FGFR over KDR is suggested to be caused by the difference in the interaction with M535 in FGFR1 and L889 in KDR[1]. The IC50 of CH5183284/Debio 1347 is 29 nM for FGF-dependent proliferation and 780 nM for VEGF-dependent proliferation[2].

In Vivo

CH5183284 treatment shows a dose-dependent tumor regression (tumor growth inhibition (TGI)=106% at 30 mg/kg and 147% at 100 mg/kg) without apparent body weight loss. CH5183284 treatment also shows significant in vivo efficacy in xenograft mice models with FGFR genetic alterations, such as KG1 (leukemia, FGFR1OP-FGFR1 fusion), MFE280 (endometrial cancer, FGFR2 S252W mutation), UM-UC-14 (bladder cancer, FGFR3 S249C mutation), and RT112/84 (bladder cancer, FGFR3-TACC3 fusion)[1].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.8060 mL 14.0300 mL 28.0599 mL
5 mM 0.5612 mL 2.8060 mL 5.6120 mL
10 mM 0.2806 mL 1.4030 mL 2.8060 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

The cell lines are added to the wells of 96-well plates containing 0.076−10,000 nM tested compounds (CH5183284) and incubated at 37°C. After 4 days’ incubation, Cell Counting Kit-8 solution is added, and after incubation for several more hours, absorbance at 450 nm is measured. The antiproliferative activity is calculated using the formula (1-T/C) × 100 (%), where T and C represent absorbance at 450 nm of the cells treated with drugs (T) and that of untreated control cells (C)[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1][2]

CH5183284 is prepared in 0.5% carmellose sodium, 0.5% polysorbate 20, and 0.9% benzyl alcohol in purified water[2].

Rat: Male Wistar rats (340–390 g) implanted with a telemetry transmitter are used for the assessment of effects on blood pressure (BP). Vehicle (0.5% carmellose sodium, 0.5% polysorbate 20, and 0.9% benzyl alcohol in purified water) or CH5183284/Debio 1347 (10 and 30 mg/kg) are administered by oral gavage once a day for 4 consecutive days. Data for blood pressure are automatically analyzed and continuously recorded at 5-minute intervals[2].

Mouse: The in vivo efficacy is evaluated in mice bearing an SNU-16 xenograft. CH5183284 is orally administered once daily for 11 days, and the body weight of mice and the volume of the tumors are measured twice a week[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

356.38

Formula

C₂₀H₁₆N₆O

CAS No.

1265229-25-1

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: ≥ 31mg/mL

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

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Product Name:
CH5183284
Cat. No.:
HY-19957
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