Referencia número: HY-101756

SDZ281-977

Name: SDZ281-977
Brand: MedChemExpress
SKU: HY-101756
Price: 300.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: SDZ-LAP 977)

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Based on 1 Customer Validation

SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 98.00%
No. CAS: 150779-71-8
Fòrmula: C₁₈H₂₀O₅
Peso molecular:316.35

Almacenamiento:

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

SDZ281-977 Chemical Structure

No. CAS: 150779-71-8

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

Actividad biológica

Descripciòn

SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A.

Ver todos los productos específicos de isoformas EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	213 nM Compound: 13	Inhibition of A431 cell proliferation Inhibition of A431 cell proliferation	[PMID: 7990108]
B16	IC₅₀	269 nM Compound: 13	Inhibition of B16F1 cell proliferation Inhibition of B16F1 cell proliferation	[PMID: 7990108]
HaCaT	IC₅₀	0.04 μM Compound: 13	Inhibitory activity of HaCaT keratinocyte cell line Inhibitory activity of HaCaT keratinocyte cell line	[PMID: 7990108]
HaCaT	IC₅₀	47 nM Compound: 1, SDZ LAP 977	Antiproliferative activity against human HaCaT cells after 3 days by sulforhodamine B assay Antiproliferative activity against human HaCaT cells after 3 days by sulforhodamine B assay	[PMID: 18678497]
HeLa	IC₅₀	470 nM Compound: 13	Inhibition of HeLa cell proliferation Inhibition of HeLa cell proliferation	[PMID: 7990108]
K562	IC₅₀	217.5 nM Compound: 13	Inhibition of K562 cell proliferation Inhibition of K562 cell proliferation	[PMID: 7990108]
KB	IC₅₀	191.5 nM Compound: 13	Inhibition of KB cell proliferation Inhibition of KB cell proliferation	[PMID: 7990108]
L1210	IC₅₀	415 nM Compound: 13	Inhibition of L1210 cell proliferation Inhibition of L1210 cell proliferation	[PMID: 7990108]
LoVo	IC₅₀	185 nM Compound: 13	Inhibition of LOVO cell proliferation Inhibition of LOVO cell proliferation	[PMID: 7990108]
MCF7	IC₅₀	19 nM Compound: 13	Inhibition of MCF-7 cell proliferation Inhibition of MCF-7 cell proliferation	[PMID: 7990108]
MDA-MB-231	IC₅₀	427.5 nM Compound: 13	Inhibition of MDA-MB-231 cell proliferation Inhibition of MDA-MB-231 cell proliferation	[PMID: 7990108]
MDA-MB-468	IC₅₀	46.5 nM Compound: 13	Inhibition of MDA-MB-468 cell proliferation Inhibition of MDA-MB-468 cell proliferation	[PMID: 7990108]
P388	IC₅₀	337.5 nM Compound: 13	Inhibition of P388 cell proliferation Inhibition of P388 cell proliferation	[PMID: 7990108]
SCL-1	IC₅₀	383 nM Compound: 13	Inhibition of SCL-1 cell proliferation Inhibition of SCL-1 cell proliferation	[PMID: 7990108]
SK-BR-3	IC₅₀	31 nM Compound: 13	Inhibition of SK-BR-3 cell proliferation Inhibition of SK-BR-3 cell proliferation	[PMID: 7990108]
U-937	IC₅₀	320 nM Compound: 13	Inhibition of U937 cell proliferation Inhibition of U937 cell proliferation	[PMID: 7990108]

In Vitro

The anticancer profile of SDZ 281-977 is investigated in nude mice bearing the human tumor cell lines A431 (vulvar carcinoma cells), MIA PaCa-2 (pancreatic tumor cells) and MDA-MB-231 (breast carcinoma cells). These cell lines are selected because of their sensitivity for SDZ 281-977. The IC₅₀ values for inhibition of growth of A431, MIA PaCa-2 and MDA-MB-231 cells are 0.21 μM, 0.29 μM and 0.43 μM, respectively^[1].

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

In Vivo

Nude mice bearing A431 human vulvar carcinomas receive intravenous injections of SDZ 281-977 (1-10 mg/kg) for 4 weeks. This treatment results in a dose-dependent inhibition of tumor growth. Orally administered SDZ 281-977 (30 mg/kg) induces a 54% inhibition of A431 tumor growth after 3 weeks of treatment. The above regimens are well tolerated. No significant change in body weight occurred during treatment^[1].

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

Chemical Information

No. CAS 150779-71-8
Appearance Solid
Peso molecular 316.35
Fòrmula C₁₈H₂₀O₅
Color White to off-white
SMILES

O=C(OC)C1=CC(CCC2=CC(OC)=CC=C2OC)=CC=C1O
Synonyms

SDZ-LAP 977
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 : 100 mg/mL (316.11 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

3.1611 mL

15.8053 mL

31.6106 mL

5 mM

0.6322 mL

3.1611 mL

6.3221 mL

10 mM

0.3161 mL

1.5805 mL

3.1611 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)

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (7.90 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocolo

Cell Assay^[1]

Tumor cell lines are grown at 37°C under optimal medium and cell concentration conditions in the absence of antibiotics. At the time of exponential growth for tumor cell lines growing in suspension or at the time of 60-90% confluence for adherent cell lines, cells are harvested (adherent cell lines are trypsinized), suspended in fresh growth medium and seeded into 96-well cell culture plates at concentrations ranging between 1000 and 5000 cells/well. Cells are grown at optimal initial concentration for 3-4 days in a final volume of 0.2 ml/well in the presence of graded concentrations of test compounds. Extent of cellular proliferation is measured by a colorimetric assay using MTT for cells growing in suspension or by sulforhodamine B (SRB) for adherent cells^[1].

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

Animal Administration^[1]

Mice^[1]
Female nude mice (nu/nu IFFA C BALB A) weighing 20-23 g are used. For i.v. studies, SDZ 281-977 (10 mg) is dissolved in 1 mL Vepesid solvent (3250 mg PEG 300, 10 mg citric acid, 400 mg Tween 80 and 1205 mg ethanol). This solution is diluted with saline or Vepesid solvent/saline 1:10 so that all animals intravenously receive 0.2 mL of 1:10 Vepesid solvent containing 1, 3 and 10 mg SDZ 281-977/kg. Higher doses are not given due to limited solubility. SDZ 281-977 is injected into the tail vein 3 or 4 times a week. For oral testing, SDZ 281-977 is dissolved in Placebo G (18% ethanol, 43% Labrafil M2125CS and 39% corn oil) and 0.2 mL is given orally with a gavage. Control animals are treated with the vehicle only. For the comparative experiments, standard anticancer drugs are dissolved in saline containing 1% Tween 80 and water, respectively, and are injected i.p. once a day for 4 days in a row. Treatment started 2 days after animals have been randomized.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Cammisuli S, et al. SDZ 281-977: a modified partial structure of lavendustin A that exerts potent and selective antiproliferative activities in vitro and in vivo. Int J Cancer. 1996 Jan 26;65(3):351-9. [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	3.1611 mL	15.8053 mL	31.6106 mL	79.0264 mL
	5 mM	0.6322 mL	3.1611 mL	6.3221 mL	15.8053 mL
	10 mM	0.3161 mL	1.5805 mL	3.1611 mL	7.9026 mL
	15 mM	0.2107 mL	1.0537 mL	2.1074 mL	5.2684 mL
	20 mM	0.1581 mL	0.7903 mL	1.5805 mL	3.9513 mL
	25 mM	0.1264 mL	0.6322 mL	1.2644 mL	3.1611 mL
	30 mM	0.1054 mL	0.5268 mL	1.0537 mL	2.6342 mL
	40 mM	0.0790 mL	0.3951 mL	0.7903 mL	1.9757 mL
	50 mM	0.0632 mL	0.3161 mL	0.6322 mL	1.5805 mL
	60 mM	0.0527 mL	0.2634 mL	0.5268 mL	1.3171 mL
	80 mM	0.0395 mL	0.1976 mL	0.3951 mL	0.9878 mL
	100 mM	0.0316 mL	0.1581 mL	0.3161 mL	0.7903 mL

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SDZ281-977

Ver todos los productos específicos de isoformas EGFR

Actividad biológica

Chemical Information

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

SDZ281-977 Related Classifications

HY-101756 Related Classifications

Bioz