TCS-359
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406289

CAS#: 301305-73-7

Description: TCS-359 is a potent inhibitor of FLT3 with IC50 of 42 nM.


Chemical Structure

img
TCS-359
CAS# 301305-73-7

Theoretical Analysis

MedKoo Cat#: 406289
Name: TCS-359
CAS#: 301305-73-7
Chemical Formula: C18H20N2O4S
Exact Mass: 360.11
Molecular Weight: 360.430
Elemental Analysis: C, 59.98; H, 5.59; N, 7.77; O, 17.76; S, 8.90

Price and Availability

Size Price Availability Quantity
25mg USD 150 Ready to ship
50mg USD 250 Ready to ship
100mg USD 450 Ready to ship
200mg USD 750 Ready to ship
500mg USD 1550 Ready to ship
1g USD 2650 Ready to ship
Bulk inquiry

Synonym: TCS359, TCS 359, TCS-359, Flt-3 inhibitor

IUPAC/Chemical Name: 2-(3,4-dimethoxybenzamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide

InChi Key: FSPQCTGGIANIJZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H20N2O4S/c1-23-12-8-7-10(9-13(12)24-2)17(22)20-18-15(16(19)21)11-5-3-4-6-14(11)25-18/h7-9H,3-6H2,1-2H3,(H2,19,21)(H,20,22)

SMILES Code: O=C(C1=C(NC(C2=CC=C(OC)C(OC)=C2)=O)SC3=C1CCCC3)N

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: TCS 359 is a FLT3 inhibitor with an IC50 of 42 nM.
In vitro activity: TCS 359 showed marked effects on eliciting imMKCL (immortalized MK [megakaryocyte] cell line) maturation, as judged by upregulated TUBB1 (β1-tubulin) levels (supplemental Figure 3C), enlarged surface area (Figure 3A), enhanced number of proplatelet-bearing MKs (supplemental Figure 4), and increased PLP (platelet-like particles) yield (Figure 2F; supplemental Figure 5). The results suggested that increased PLP production results from a higher number of MKs that extend proplatelets rather than a higher degree of MK maturation. The structure of PLPs produced under the addition of TCS 359 using transmission electron microscopy (supplemental Figure 6) were evaluated and it was confirmed that the levels of PAC-1 binding were comparable with human donor–derived platelets (Figure 3C). Reference: Blood Adv. 2018 Sep 11;2(17):2262-2272. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6134216/
In vivo activity: Whether Wnt-C59 and TCS 359 could improve in vivo thrombopoiesis was studied using a mouse thrombocytopenia model induced by the administration of anti-GPIbα antibody (200 ng/g body weight; Figure 3F). Because SR1 is a human specific AhR antagonist, the actions of Wnt-C59, TCS 359, and CH223191, an AhR antagonist nonselective for species, were evaluated. The 3 drugs showed a significant tendency to recover platelet levels compared with the control (phosphate-buffered saline; PBS) group (Figure 3G; supplemental Figure 8), suggesting that thrombocytopenia in mice was better restored by the 3 drugs. Reference: Blood Adv. 2018 Sep 11;2(17):2262-2272. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6134216/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.8 29.91
DMF 5.0 13.87
DMF:PBS (pH 7.2) (1:3) 0.3 0.69

Preparing Stock Solutions

The following data is based on the product molecular weight 360.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Seo H, Chen SJ, Hashimoto K, Endo H, Nishi Y, Ohta A, Yamamoto T, Hotta A, Sawaguchi A, Hayashi H, Koseki N, Murphy GJ, Fukuda K, Sugimoto N, Eto K. A β1-tubulin-based megakaryocyte maturation reporter system identifies novel drugs that promote platelet production. Blood Adv. 2018 Sep 11;2(17):2262-2272. doi: 10.1182/bloodadvances.2018019547. PMID: 30206099; PMCID: PMC6134216.
In vitro protocol: 1. Seo H, Chen SJ, Hashimoto K, Endo H, Nishi Y, Ohta A, Yamamoto T, Hotta A, Sawaguchi A, Hayashi H, Koseki N, Murphy GJ, Fukuda K, Sugimoto N, Eto K. A β1-tubulin-based megakaryocyte maturation reporter system identifies novel drugs that promote platelet production. Blood Adv. 2018 Sep 11;2(17):2262-2272. doi: 10.1182/bloodadvances.2018019547. PMID: 30206099; PMCID: PMC6134216.
In vivo protocol: 1. Seo H, Chen SJ, Hashimoto K, Endo H, Nishi Y, Ohta A, Yamamoto T, Hotta A, Sawaguchi A, Hayashi H, Koseki N, Murphy GJ, Fukuda K, Sugimoto N, Eto K. A β1-tubulin-based megakaryocyte maturation reporter system identifies novel drugs that promote platelet production. Blood Adv. 2018 Sep 11;2(17):2262-2272. doi: 10.1182/bloodadvances.2018019547. PMID: 30206099; PMCID: PMC6134216.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Patch RJ, Baumann CA, Liu J, Gibbs AC, Ott H, Lattanze J, Player MR. Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3282-6. Epub 2006 Mar 31. PubMed PMID: 16580199.