Referencia número: HY-100434

PD-161570

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Based on 1 Customer Validation

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC₅₀ of 39.9 nM and a K_i of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC₅₀ values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC₅₀s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.

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Pureza: 99.82%
No. CAS: 192705-80-9
Fòrmula: C₂₆H₃₅Cl₂N₇O
Peso molecular:532.51

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PD-161570 Chemical Structure

No. CAS: 192705-80-9

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Precio

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Amount: USD 0.00

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC₅₀ of 39.9 nM and a K_i of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC₅₀ values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC₅₀s of 450 nM and 622 nM, respectively^[1]^[2]. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor^[3].

IC₅₀ & Target^[1]^[2]^[3]

FGFR1

39.9 nM (IC₅₀)

FGFR1

42 nM (Ki)

FGFR1 autophosphorylation

622 nM (IC₅₀)

PDGFRβ

262 nM (IC₅₀)

PDGFR

310 nM (IC₅₀)

EGFR

240 nM (IC₅₀)

c-Src

44 nM (IC₅₀)

TGF-β Receptor

Ver todos los productos específicos de isoformas PDGFR :

Ver todos los productos específicos de isoformas EGFR :

Ver todos los productos específicos de isoformas Src :

Ver todos los productos específicos de isoformas TGF-β Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
C6	IC₅₀	5.8 μM Compound: 33	Inhibition of C-6 rat glioma cell proliferation Inhibition of C-6 rat glioma cell proliferation	[PMID: 11384237]
HCT-8	IC₅₀	16.3 μM Compound: 33	Inhibition of human colon carcinoma HCT-8 cell proliferation Inhibition of human colon carcinoma HCT-8 cell proliferation	[PMID: 11384237]
HT-29	IC₅₀	0.9 μM Compound: 33	Inhibition of human colon carcinoma HT-29 cell proliferation Inhibition of human colon carcinoma HT-29 cell proliferation	[PMID: 11384237]
SW-620	IC₅₀	>25 μM Compound: 33	Inhibition of human colon carcinoma SW-620 cell proliferation Inhibition of human colon carcinoma SW-620 cell proliferation	[PMID: 11384237]

In Vitro

PD-161570 (Compound 6c; 0.1-1 μM; 1-8 days; VSMCs) treatment inhibits PDGF-stimulated vascular smooth muscle cell proliferation in a dose dependent fashion with an IC₅₀ of 0.3 μM on day 8^[1].
PD-161570 suppresses constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A_121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A_121(p) cells in culture^[2].
PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis^[4].

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

Cell Proliferation Assay^[1]

Cell Line:

Vascular smooth muscles cells (VSMCs)
Concentration:

0.1 µM, 0.3 µM, 1 µM
Incubation Time:

1 day, 3 days, 6 days, 8 days
Result:

Inhibited VSMC proliferation in a dose dependent fashion with an IC₅₀ of 0.3 µM at day 8.

Chemical Information

No. CAS 192705-80-9
Appearance Solid
Peso molecular 532.51
Fòrmula C₂₆H₃₅Cl₂N₇O
Color Light yellow to yellow
SMILES

O=C(NC(C)(C)C)NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=C(Cl)C=CC=C3Cl
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 33.33 mg/mL (62.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8779 mL

9.3895 mL

18.7790 mL

5 mM

0.3756 mL

1.8779 mL

3.7558 mL

10 mM

0.1878 mL

0.9389 mL

1.8779 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (275 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Hamby JM, et al. Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. J Med Chem. 1997 Jul 18;40(15):2296-303. [Content Brief]

[2]. Batley BL, et al. Inhibition of FGF-1 receptor tyrosine kinase activity by PD 161570, a new protein-tyrosine kinase inhibitor. Life Sci. 1998;62(2):143-50. [Content Brief]

[3]. Kyosuke Hino, et al. An mTOR Signaling Modulator Suppressed Heterotopic Ossification of Fibrodysplasia Ossificans Progressiva. Stem Cell Reports. 2018 Nov 13;11(5):1106-1119. [Content Brief]

[4]. Wolfe A, et al. Pharmacologic characterization of a kinetic in vitro human co-culture angiogenesis model using clinically relevant compounds. J Biomol Screen. 2013 Dec;18(10):1234-45. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8779 mL	9.3895 mL	18.7790 mL	46.9475 mL
	5 mM	0.3756 mL	1.8779 mL	3.7558 mL	9.3895 mL
	10 mM	0.1878 mL	0.9389 mL	1.8779 mL	4.6947 mL
	15 mM	0.1252 mL	0.6260 mL	1.2519 mL	3.1298 mL
	20 mM	0.0939 mL	0.4695 mL	0.9389 mL	2.3474 mL
	25 mM	0.0751 mL	0.3756 mL	0.7512 mL	1.8779 mL
	30 mM	0.0626 mL	0.3130 mL	0.6260 mL	1.5649 mL
	40 mM	0.0469 mL	0.2347 mL	0.4695 mL	1.1737 mL
	50 mM	0.0376 mL	0.1878 mL	0.3756 mL	0.9389 mL
	60 mM	0.0313 mL	0.1565 mL	0.3130 mL	0.7825 mL

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PD-161570

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

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Protein Tyrosine Kinase Compound Library

TGF-beta/Smad Compound Library

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Posttranslational Modification Library

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Ver todos los productos específicos de isoformas PDGFR

Ver todos los productos específicos de isoformas EGFR

Ver todos los productos específicos de isoformas Src

Ver todos los productos específicos de isoformas TGF-β Receptor

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PD-161570 Related Classifications

HY-100434 Related Classifications