2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR-IN-26

FGFR-IN-26 is an orally active FGFR inhibitor. FGFR-IN-26 inhibits FGFR2 wild-type and clinically relevant resistance mutations. FGFR-IN-26 inhibits tumor growth in FGFR2-amplified xenograft mouse models. FGFR-IN-26 can be used for the research of cancer, suah as gastric carcinoma.

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

FGFR-IN-26

FGFR-IN-26 Chemical Structure

CAS No. : 2823290-68-0

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FGFR-IN-26 Related Antibodies

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Description

FGFR-IN-26 is an orally active FGFR inhibitor. FGFR-IN-26 inhibits FGFR2 wild-type and clinically relevant resistance mutations. FGFR-IN-26 inhibits tumor growth in FGFR2-amplified xenograft mouse models. FGFR-IN-26 can be used for the research of cancer, suah as gastric carcinoma[1].

IC50 & Target[1]

FGFR3

0.2 nM (IC50)

FGFR2

2.1 nM (IC50)

FGFR1

3.8 nM (IC50)

FGFR4

49 nM (IC50)

In Vitro

FGFR-IN-26 (Compound 13) (dose-response series) potently inhibits proliferation of Ba/F3 cells expressing FGFR1, FGFR2 (wild-type and clinically relevant resistance mutations), FGFR3, and FGFR4, with highest potency against FGFR2K660E (IC50 = 0.6 nM) and FGFR3 (IC50 = 0.2 nM) and 23-fold selectivity for FGFR2 over FGFR4[1].
FGFR-IN-26 binds potently to FGFR2 (Kd = 2.7 nM), FGFR2(N550K) (Kd = 10 nM), FGFR1 (Kd = 21 nM), and FGFR3 (Kd = 3.5 nM), with 85-fold selectivity for FGFR2 over FGFR4, and shows weak reversible binding to FGFR2(C491F) (Kd = 956 nM) consistent with a covalent mechanism[1].
FGFR-IN-26 (72-120 h) potently inhibits viability of FGFR2-driven SNU-16 gastric cancer cells (IC50 = 7.5 nM) and AN3CA endometrial cancer cells harboring FGFR2N550K (IC50 = 13 nM)[1].
FGFR-IN-26 (1 μM) shows high selectivity against the human kinome, inhibiting only 13 wild-type kinases by >90%[1].

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

FGFR-IN-26 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 AUClast Cmax F Vd CL
Rat[1] 2 mg/kg i.v. 0.7 h 1032 ng·h/mL / / 0.8 L/kg 32 mL/min/kg
Rat[1] 10 mg/kg p.o. 2.4 h 1069 ng·h/mL 352 ng/mL 21 % / /
In Vivo

FGFR-IN-26 (Compound 13) (10 mg/kg; p.o.; twice daily; 21 days) achieves 152% tumor growth inhibition in an FGFR2-amplified SNU-16 gastric carcinoma xenograft model in nude mice, with no significant body weight loss[1].

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

Animal Model: FGFR2-amplified SNU-16 gastric carcinoma xenograft model in nude mice (female, 6-8-week-old)[1]
Dosage: 10 mg/kg
Administration: p.o.; twice daily; 21 days
Result: Achieved 152% tumor growth inhibition (TGI) over 21 days.
Reached a terminal day 21 plasma level of 192 ng/mL (480 nM) 4 h after the final dose.
Caused no significant body weight loss after 21 days.
Molecular Weight

401.46

Formula

C22H23N7O
CAS No.
SMILES

C=CC(NC1=CC2=C(C=C1)C(C3=NC(NC4=CN(C(C)C)N=C4)=NC=C3)=CN2C)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FGFR-IN-26 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FGFR-IN-262823290-68-0FGFRFibroblast growth factor receptorFGFR3intrahepatic cholangiocarcinomagastric carcinomaFGFR1endometrial cancerFGFR4FGFR2SNU-16Ba/F3 cellsAN3CAInhibitorinhibitorinhibit

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