SW106065 is an inducer of apoptosis in malignant peripheral nerve sheath tumors (MPNST). SW106065 inhibits ATP consumption by MPNST in sMPNST cells and other models with EC50 of 1 µM. SW106065 can be used for MPNST research.

Physicochemical Properties

Molecular Formula	C10H8N2OS
Molecular Weight	204.25
Exact Mass	204.036
CAS #	62289-81-0
Related CAS #	62289-81-0
PubChem CID	790407
Appearance	Solid
LogP	2.468
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	2
Heavy Atom Count	14
Complexity	210
Defined Atom Stereocenter Count	0
SMILES	C1=CC(=CN=C1)NC(=O)C2=CC=CS2
InChi Key	UPLHUDRMLWWFRE-UHFFFAOYSA-N
InChi Code	InChI=1S/C10H8N2OS/c13-10(9-4-2-6-14-9)12-8-3-1-5-11-7-8/h1-7H,(H,12,13)
Chemical Name	N-pyridin-3-ylthiophene-2-carboxamide
Synonyms	SW 106065; SW-106065; SW106065; MPNST-IN-21
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	SW106065 (Compound 21, Cpd21) inhibits the growth of human MPNST cell lines in a dose-dependent manner, with EC50 values for S462 and SNF96.2 cells of 439 nM and 753.6 nM, respectively. To normally dividing Schwann cells or mouse embryonic fibroblasts, SW106065 is still nontoxic[1]. SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment shows a decreased percentage of cells in S phase and an increase in the proportion of G1/G0 and G2/M cells[1]. SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment decreases the levels of cyclin A2, cyclin B1, cyclin D1, cyclin E, cdk4, and cdk6. Additionally, a dose-dependent increase in mRNA levels for CDKN1A and CDKN2A was seen. SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment decreases the levels of Cyclin D1 protein[1]. SW106065 (Cpd21) treatment significant increase in the percentage of apoptotic cells[1].
ln Vivo	SW106065 (Cpd21; 40 mg/kg; intraperitoneal injection; twice per day for 4 weeks) treatment can be given to mice in concentrations that sufficiently penetrate sMPNST tissue and prevent tumor growth[1].
References	[1]. Preclinical therapeutic efficacy of a novel pharmacologic inducer of apoptosis in malignant peripheral nerve sheath tumors. Cancer Res. 2014 Jan 15;74(2):586-97.

Solubility Data

Solubility (In Vitro)

DMSO: 41~100 mg/mL (200.7~489.6 mM) Ethanol: ~41 mg/mL (~200.7 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (12.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (12.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.8960 mL	24.4798 mL	48.9596 mL
	5 mM	0.9792 mL	4.8960 mL	9.7919 mL
	10 mM	0.4896 mL	2.4480 mL	4.8960 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.