PD-166866

Name: PD-166866
Brand: MedChemExpress
SKU: HY-101296
Rating: 5.0 (11 reviews)

Cat. No.: HY-101296 Purity: 99.75%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC₅₀ of 52.4 nM.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

PD-166866 화학구조

CAS No. : 192705-79-6

사이즈	재고	수량
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
500 mg	해외재고보유	Estimated Time of Arrival: December 31
1 g	해외재고보유	Estimated Time of Arrival: December 31
5 g	견적 받기
10 g	견적 받기

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고객리뷰

Based on 11 publication(s) in Google Scholar

Other Forms of PD-166866:

PD-166866 (Standard) 견적 받기

11 Publications Citing Use of MCE PD-166866

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•Related Screening Libraries:

•Related Small Molecules:

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Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC₅₀ of 52.4 nM.

IC₅₀ & Target^[1]

FGFR1

52.4 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
C6	IC₅₀	>25 μM Compound: 5	Inhibition of PDGF-dependent rat glioma C6 cell proliferation Inhibition of PDGF-dependent rat glioma C6 cell proliferation	[PMID: 11063616]
HUVEC	IC₅₀	0.1 μM Compound: 5	Inhibition of microcapillary growth in HUVEC cells Inhibition of microcapillary growth in HUVEC cells	[PMID: 11063616]
HUVEC	IC₅₀	0.58 μM Compound: 5	Inhibition of in vitro cell Human umbilical vein endothelial (HUVEC) cell proliferation Inhibition of in vitro cell Human umbilical vein endothelial (HUVEC) cell proliferation	[PMID: 11063616]
HUVEC	IC₅₀	1.1 μM Compound: 5	Inhibition of Matrigel invasion assay in HUVEC cells Inhibition of Matrigel invasion assay in HUVEC cells	[PMID: 11063616]
Ovarian cancer cell line	IC₅₀	15 μM Compound: 5	Inhibition of human ovarian carcinoma (A90) FGF-R overexpressing cell proliferation Inhibition of human ovarian carcinoma (A90) FGF-R overexpressing cell proliferation	[PMID: 11063616]

In Vitro

PD 166866 inhibits human full-length FGFR-1 tyrosine kinase with an IC₅₀ value of 52.4 nM and is characterized as an ATP competitive inhibitor of the FGFR-1. PD 166866 is a potent inhibitor of FGFR autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and in L6 cells overexpressing the human FGFR-1 tyrosine kinase. PD 166866 also inhibits bFGF-induced tyrosine phosphorylation of the 44- and 42-kDa (ERK 1/2) mitogen-activated protein kinase isoforms in L6 cells. Daily exposure of PD 166866 to L6 cells at concentrations from 1 to 100 nM results in a concentration-related inhibition of bFGF-stimulated cell growth for 8 consecutive days with an IC₅₀ value of 24 nM^[1].

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

분자량

396.44

화학식

C₂₀H₂₄N₆O₃

CAS No.

192705-79-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC(C)(C)C)NC1=NC2=NC(N)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

In Vitro:

DMSO : 3.33 mg/mL (8.40 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5224 mL	12.6122 mL	25.2245 mL
5 mM	0.5045 mL	2.5224 mL	5.0449 mL
10 mM	---	---	---

View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.52 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (2.52 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 3.33 mg/mL (8.40 mM); Suspended solution; Need ultrasonic and warming and heat to 40°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.75%

Select Batch:

Data Sheet (277 KB) SDS (396 KB)

COA (251 KB) HNMR (251 KB) RP-HPLC (254 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. Panek RL, et al. In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase. J Pharmacol Exp Ther. 1998 Jul;286(1):569-77. [Content Brief]

[2]. Thompson AM, Connolly CJ, Hamby JM, et al. 3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase. J Med Chem. 2000;43(22):4200-4211. [Content Brief]

Cell Assay
^[1]

PD 166866 is dissolved in DMSO. PD 166866 or vehicle (0.5% DMSO, final concentration) are added every day to triplicate cultures of cells together with 25 ng/mL bFGF to stimulate FGF-driven growth. In some experiments, PD 166866 is added every day to triplicate cultures of cells together with 30 ng/mL PDGF-BB to stimulate PDGF-driven growth. Cell number is measured by Coulter counting on days 1, 3, 6 or 8 after drug exposure^[1]

MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.

References

[1]. Panek RL, et al. In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase. J Pharmacol Exp Ther. 1998 Jul;286(1):569-77. [Content Brief]

[2]. Thompson AM, Connolly CJ, Hamby JM, et al. 3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase. J Med Chem. 2000;43(22):4200-4211. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5224 mL	12.6122 mL	25.2245 mL	63.0612 mL
DMSO	5 mM	0.5045 mL	2.5224 mL	5.0449 mL	12.6122 mL

PD-166866 Related Classifications

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:

PD-166866192705-79-6PD166866PD 166866FGFRAutophagyFibroblast growth factor receptorInhibitorinhibitorinhibit

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PD-166866

고객리뷰

Other Forms of PD-166866:

PD-166866 Related Antibodies

11 Publications Citing Use of MCE PD-166866

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

순도&문서

References

고객리뷰

PD-166866 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

PD-166866 Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report