2. TGF-beta/Smad
  3. TGF-β Receptor
  4. TGFβRI-IN-4

TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

TGFβRI-IN-4

TGFβRI-IN-4 화학구조

CAS No. : 2421135-03-5

사이즈 재고
50 mg   견적 받기  
100 mg   견적 받기  
250 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

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

TGFβRI-IN-4 Related Antibodies

Top Publications Citing Use of Products

View All TGF-β Receptor Isoform Specific Products:

View All Isoforms
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP GDF15

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model[1].

IC50 & Target

IC50: 44 nM (ALK5), 42.5 nM (NIH3T3)[1]
In Vivo

TGFβRI-IN-4 (compound 15r) (60 mg/kg; PO; BID, for 21 days) efficiently suppresses tumor growth and tumor weight in tumor xenograft model[1].
TGFβRI-IN-4 (1 mg/kg and 10 mg/kg; IV and PO; single) exhibits good oral plasma exposure and excellent bioavailability[1].
Pharmacokinetic Parameters of TGFβRI-IN-4 in male Sprague-Dawley rats[1].

IV (1 mg/kg) PO (10 mg/kg)
T1/2 (h) 0.5 1.8
CL (L/h/kg) 4.9
Cmax (ng/mL) 926.0
VSS (L/kg) 3.0
AUC0-24 (ng/mL·h) 195.2 2351.2
F (%) 120.5%

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

Animal Model: Female BALB/C mice (5-8 weeks; injected with CT26 cells)[1]
Dosage: 60 mg/kg
Administration: PO; BID, for 21 days
Result: Efficiently suppressed tumor growth (tumor growth inhibition = 65.7%) and tumor weight.
Animal Model: Male BALB/C mice[1]
Dosage: 1 mg/kg and 10 mg/kg
Administration: IV and PO; single (Pharmacokinetic Analysis)
Result: Exhibited good oral plasma exposure and excellent bioavailability with AUC >2000 h·ng/mL and F > 80%, respectively.
분자량

441.47

화학식

C23H25F2N5O2
CAS No.
SMILES

CC(O)(C1=CC(NC2=CC(OC3=CN(N=C3C4CC(F)(C4)F)C5CC5)=CC=N2)=CC=N1)C
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.

TGFβRI-IN-4 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:

TGFβRI-IN-42421135-03-5TGF-β ReceptorTransforming growth factor beta receptorsAntitumorTumor xenograft modelBALB/C miceALK5NIH3T3Orally activeInhibitorinhibitorinhibit

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:
TGFβRI-IN-4
Cat. No.:
HY-146780
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.