TCS-359
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MedKoo CAT#: 406289

CAS#: 301305-73-7

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


Chemical Structure

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TCS-359
CAS# 301305-73-7

Theoretical Analysis

MedKoo Cat#: 406289
Name: TCS-359
CAS#: 301305-73-7
Chemical Formula: C18H20N2O4S
Exact Mass: 360.11438
Molecular Weight: 360.43
Elemental Analysis: C, 59.98; H, 5.59; N, 7.77; O, 17.76; S, 8.90

Price and Availability

Size Price Availability Quantity
25.0mg USD 150.0 Ready to ship
50.0mg USD 250.0 Ready to ship
100.0mg USD 450.0 Ready to ship
200.0mg USD 750.0 Ready to ship
500.0mg USD 1550.0 Ready to ship
1.0g USD 2650.0 Ready to ship
2.0g USD 4650.0 Ready to ship
5.0g USD 6950.0 Ready to ship
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Synonym: TCS359, TCS 359, TCS-359

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

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 10.78 29.91
DMF 5.0 13.87
DMF:PBS (pH 7.2) (1:3) 0.25 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.

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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.

TCS-359

25.0mg / USD 150.0