Chemdea
 
작성일 : 14-06-14
[Chemdea] Tyrosin kinase inhibitors


Tyrosin kinase inhibitors

 

 

Product Name: PDGFR Tyrosine Kinase Inhibitor IV (RWJ 540973, JNJ-10198409)

 

   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요

 

A cell-permeable indenopyrazole compound that displays potent antiproliferativeproperties in several human

tumor cell lines (IC50 <33 nM). Shown to act as an ATP-competitive and reversible inhibitor of PDGFR (IC50=

4.2 nM and 45 nM for -β and -α, respectively) and c-Abl (IC50 = 22 nM).Exhibits less activity towards Lck, c-Src,

and Fyn(IC50 = 100 nM, 185 nM and 378 nM, respectively) and exhibits little or noinhibition toward VEGFR, HER-2,

Cdk's-1,-2,-4 &-7, bFGFR-1 and EGFR (IC50 = 3.1 µM, >10 µM, >10 µM, 45.8 µM and >100 µM, respectively).

 

Details

Chemical Formula:

 

C18H16FN3O2

CAS No.:

 

627518-40-5

Molecular weight:

 

325.3.

Purity:

99% by HPLC

Appearance:

 

Off-White solid

Chemical name:

 

3-Fluoro-N-(6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine

Solubility:

 

DMSO (10 mg/mL) and methanol (5 mg/mL).

Storage:

Protect from light. Packaged under inert gas

 

References

 

Product Name: PD173074 – FGF/VEGF Receptor Tyrosine Kinase Inhibitor

 

   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요

 

A cell-permeable pyridopyrimidine compound that acts as a potent, ATP-competitive, and reversible inhibitor of

FGF and VEGF receptors (IC50 = 21.5 nM for FGFR1). It inhibits PDGFR and c-Src only at muchhigher

concentration (IC50 = 17.6 µM, 19.8 µM, respectively) and exhibits little effect against EGFR, InsR, MEK, andcPKC

even at concentrations as high as 50 µM. Shown to inhibit the autophosphorylation of endogenous FGFR1 (IC50

<5 nM) and overexpressed VEGFR2 (IC50 <200 nM) in NIH3T3 cells in vitro, and FGF- andVEGF-induced

angiogenesis in mice in vivo.

 

Details

Chemical Formula:

 

C28H41N7O3

CAS No.:

 

219580-11-7

Molecular weight:

 

523.7

Purity:

99% by HPLC

Appearance:

 

Yellow solid

Chemical name:

 

1-t-Butyl-3-(6-(3,5-dimethoxyphenyl)-2-(4-diethylaminobutylamino)-pyrido[2,3-d]

pyrimidin-7-yl)urea

Solubility:

 

DMSO (100 mg/mL)

Storage:

Protect from light. Packaged under inert gas

 

References

 

 

Product Name: PP1 – Src Inhibitor

   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요

 

A cell-permeable pyrazolopyrimidine compound that is shown to inhibit Src family tyrosine kinases Lck, Fyn, Hck,

and Src (IC50 = 5, 6, 20, and 170 nM, respectively), as well as non-Src family kinasessuch as CSK, RIP2, and

CK1δ (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µM, in vitro kinaseactivity is

reduced by more than 57% for p38α, p38β, CK1δ, CSK, RIP2, and GAK, while exhibiting muchlower activity

against more than 60 other kinases. Kinetic studies employing Src and [poly Glu-Tyr4:1] indicate that the

inhibition is mixed competitive with respect to the substrate and non-competitive with respect toATP. PP1 also

demonstrates anti-growth properties in several B lymphoma cultures of human and murine origins (IC50= 2.5 to

8.0 µM) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 µM).

 

Details

Chemical Formula:

 

C16H19N5

CAS No.:

 

172889-26-8

Molecular weight:

 

281.36

Purity:

99% by HPLC

Appearance:

 

White solid

Chemical name:

 

4-Amino-5-(4-methylphenyl)-7-(t-butyl)pyrazolo-d-3,4-pyrimidine

Solubility:

 

DMSO (25 mg/mL)

Storage:

Protect from light. Packaged under inert gas

 

References

 

 

Product Name: pp121 – Tyrosin Kinase and PI3K Pathway Inhibitor

 

   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요

 

A cell-permeable pyrazolopyrimidinecompound that effectively targets the ATP pocket of both protein tyrosine

kinases (IC50 <0.26 μM against Abl, EGFR, EphB4, Hck, PDGFR, RET, Src, Src, andVEGFR2) and PI3-K T338I

family kinases (IC50 <1.4 μM against p110α/β/δ/γ, mTOR, and DNA-PK).PP121 is less effective against ser/thr

kinases and exhibits significant inhibition of only 14 ser/thr kinases (70% inhibition with 1 μM inhibitor and 10 mM

ATP) in a 219 kinase panel screening. Individually targeting Ret by sorafenib (IC50 = 780 nM) or PI3-K/mTOR

pathway by PI-103 (IC50 = 800 nM) is shown to be less effective than PP121 treatment (IC50 = 50 nM) in inhibiting

the proliferation of Ret C634W-expressing TT thyroid carcinoma cultures. 

 

Details

Chemical Formula:

 

C17H17N7

CAS No.:

 

1092788-83-4

Molecular weight:

 

319.4

Purity:

99% by HPLC

Appearance:

 

White solid

Chemical name:

 

 1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1Hpyrazolo[3,4-d]pyrimidin-4-amine

Solubility:

 

(100 mg/mL), ethanol (50 mg/mL).

Storage:

Protect from light. Packaged under inert gas

 

Reference

 

Product Name: VEGFR Tyrosine Kinase Inhibitor II

 

   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요

 

A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit

(IC50 = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC50= 7.0 µM

and 7.3 µM). Also displays antiangiogenic and antitumor properties. Does not inhibit the activities ofCDK-1,

c-Met, IGF-1R or PKA (IC50 > 10 µM).

 

Details

Chemical Formula:

 

C19H16ClN3O

CAS No.:

 

269390-69-4

Molecular weight:

 

337.8

Purity:

> 99% by HPLC.

Appearance:

 

White solid

Chemical name:

 

N-(4-Chlorophenyl)-2-[(pyridin-4-ylmethyl)amino]benzamide

Solubility:

 

DMSO (5mg/mL)

Storage:

Protect from light. Packaged under inert gas

 

Reference

 

 

Ordering informations

 

Catalog No.

Product Name

Size

CD0165

PDGFR Tyrosine Kinase Inhibitor IV

(RWJ 540973, JNJ-10198409)

1mg, 5mg, 10mg, 25mg

& 50mg

CD0172

PD173074 – FGF/VEGFReceptor

Tyrosine Kinase Inhibitor

1mg, 5mg, 10mg, 25mg,

50mg, 100mg, 200mg,

250mg, 500mg & 1g

CD0334

PP1 – Src Inhibitor

1mg, 5mg, 10mg, 25mg,

50mg & 100mg

CD0257

pp121 – Tyrosin Kinase and PI3K Pathway Inhibitor

1mg, 5mg, 10mg, 25mg,

50mg ,100mg & 200mg

CD0207

VEGFR Tyrosine Kinase Inhibitor II

1mg, 5mg, 10mg, 25mg, 

50mg & 100mg

 

 

▣ 관련 페이지 ; Chemdea