2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR2/3-IN-1

FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

FGFR2/3-IN-1

FGFR2/3-IN-1 화학구조

CAS No. : 2640352-86-7

사이즈 재고
1 mg 견적 받기

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

FGFR2/3-IN-1 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].

Application

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

IC50 & Target[1]

FGFR2

1 nM (IC50)

FGFR3

0.5 nM (IC50)

FGFR3 V555L

2.7 nM (IC50)

FGFR3 V555M

6.1 nM (IC50)

FGFR1

21 nM (IC50)

FGFR4

145 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
0.5 nM
Compound: 29
Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
[PMID: 36356320]
Sf9 IC50
1 nM
Compound: 29
Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
[PMID: 36356320]
In Vitro

FGFR2/3-IN-1 (compound 29) has a clean CYP profile (CYP3A4 IC50 >25 μM). FGFR2/3-IN-1 displays excellent potency (whole blood, IC50 = 177 nM) in a whole blood (WB) assay[1].

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

FGFR2/3-IN-1 Related Antibodies
In Vivo

FGFR2/3-IN-1 (compound 29) is advanced into rat pharmacokinetics studies. Clearance in the i.v. arm is low (hepatic blood flow (HBF) = 35%), with a moderate half-life (t1/2 = 1.7 h). In the p.o. dose, FGFR2/3-IN-1 demonstrates good exposure (AUC = 5108 nM·h) and high oral bioavailability (F% = 82)[2].

rat i.v. rat p.o.
dose (mg/kg) 1.0 dose (mg/kg) 3.0
HBF% 35 Cmax (nM) 2303
Vdss (L/kg) 1.6 AUC (nM·h) 5108
T1/2 (h) 1.7 F% 82

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

450.51

화학식

C23H22D3N7O3
CAS No.
SMILES

[2H]C([2H])(NC(C1=CC(C2=C3N=C(C(C4=CN(N=C4)C(C)C)=CN3N=C2)O[C@@H]5COCC5)=CN=C1)=O)[2H]
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

FGFR2/3-IN-1 Related Classifications

  • 몰농도 계산기

  • 농도 희석 계산기

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

FGFR2/3-IN-12640352-86-7FGFRFibroblast growth factor receptorFGFR2FGFR3FGFR3 V555LFGFR3 V555Moral bioavailabilityInhibitorinhibitorinhibit

최근 본 상품:

온라인 문의

Your information is safe with us. * Required Fields.

상품명

  

Requested Quantity *

고객명 *

 

호칭

메일주소 *

 

전화번호 *

Department

 

회사명 *

City

도

Country or Region *

      

비고

대량구매 문의

Inquiry Information

상품명:
FGFR2/3-IN-1
Cat. No.:
HY-151903S
수량:
MCE Japan Authorized Agent:

고객리뷰

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

상품명

  

Lot #

고객명 *

 

메일주소 *

전화번호

 

Department *

회사명 *

 

Country or Region *

비고

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.