SDZ281-977 (Synonyms: SDZ-LAP 977)

Cat. No.: HY-101756: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

SDZ281-977 Chemical Structure

CAS No. : 150779-71-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 330	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 330	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 980	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2400	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

Cellular Effect

Cell Line	Type	Value	Description	References
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]

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.

Molecular Weight

316.35

Formula

C₁₈H₂₀O₅

CAS No.

150779-71-8

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
Dilution Calculator

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 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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 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

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.

Purity & Documentation

Purity: 98.00%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (246 KB) HNMR (253 KB) LCMS (265 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

SDZ281-977 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:

SDZ281-977150779-71-8SDZ-LAP 977EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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