1. Protein Tyrosine Kinase/RTK
  2. FGFR

FIIN-2 

Cat. No.: HY-18602
Handling Instructions

FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.

For research use only. We do not sell to patients.
FIIN-2 Chemical Structure

FIIN-2 Chemical Structure

CAS No. : 1633044-56-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO $142 In-stock
5 mg $102 In-stock
10 mg $160 In-stock
25 mg $320 In-stock
50 mg $550 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • References

Description

FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively. IC50 value: 3.1, 4.3, 27, and 45 nM [1] Target: FGFR1-4 in vitro: FIIN-2 also moderately inhibits EGFR, with an IC50 of 204 nM. The Cys491 of FGFR2 is the primary labeled site for FIIN-2 binding. FIIN-2 is the first class of inhibitors that can potently inhibit the proliferation of cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2. The co-crystal structure of FGFR4 with FIIN-2 was reported, which unexpectedly exhibits a "DFG-out" covalent binding mode. FIIN-2 maintains the pyrimido[4,5-d] pyrimidinone core of FIIN-1 but removes the two chlorine atoms, which are crucial for FIIN-1's potency against FGFR. FIIN-2 maintains the ability to form a covalent bond with the P-loop cysteine but alter the selectivity profile versus other kinases. Compared with FIIN-1, FIIN-2 displays strong binding to FGFRs and exhibited good overall kinase selectivity. FIIN-2 exhibits much less affinity for EGFR, but FIIN-3 potently bound to WT EGFR and to a subset of EGFR mutants. FIIN-2 inhibits proliferation of FGFR1-4 Ba/F3 cells with EC50s in the nanomolar range and were especially potent against FGFR2, with EC50s in the 1-nM range. FIIN-2 also inhibited the FGFR2 V564M gatekeeper mutant Ba/F3 cells, with EC50s of 58 nM, whereas FIIN-1 and BGJ398 had EC50s of over 1.0 μM against this mutant. FIIN-2 showed good potency against gatekeeper mutant V564F. In contrast, FIIN-2 was fourfold less potent (EC50 of 506 nM). FIIN-2 was inactive up to a concentration of 1.8 μM against EGFR L858R. FIIN-2 showed rather poor potency against protein kinase FLT1 (FLT1). In WT FGFR2 Ba/F3 cells, FIIN-2 completely inhibits the FGFR2 autophosphorylation on mutations of Tyr656/657 and V564M at concentrations of 3 nM and 300 nM, respectively. [1]

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.5755 mL 7.8774 mL 15.7547 mL
5 mM 0.3151 mL 1.5755 mL 3.1509 mL
10 mM 0.1575 mL 0.7877 mL 1.5755 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

634.73

Formula

C₃₅H₃₈N₈O₄

CAS No.

1633044-56-0

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: ≥ 30 mg/mL

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

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
FIIN-2
Cat. No.:
HY-18602
Quantity: