TCS-359 | CAS#301305-73-7 | FLT-3 Inhibitor

MedKoo Cat#: 406289 | Name: TCS-359

Description:

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

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

Chemical Structure

TCS-359

CAS#301305-73-7

Theoretical Analysis

MedKoo Cat#: 406289

Name: TCS-359

CAS#: 301305-73-7

Chemical Formula: C18H20N2O4S

Exact Mass: 360.1144

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
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 750.00	Ready to ship
500mg	USD 1,550.00	Ready to ship
1g	USD 2,650.00	Ready to ship

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Related CAS #

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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

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A9T06K12

QC Data

View QC data: current batch, Lot#A9T06K12

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

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/

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

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

In vivo protocol:

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.