CH7057288 | CAS# 2095616-82-1 | Selective TRK Inhibitor

MedKoo Cat#: 573171 | Name: CH7057288

Description:

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

CH7057288 is a selective TRK inhibitor that may be useful in inhibiting TRK fusion-positive cancer cell growth. TRK receptor tyrosine kinases are expressed as fusion proteins encoded by various fusion genes across a wide variety of cancer types, including lung and colorectal cancer.

Chemical Structure

CH7057288

CAS#2095616-82-1

Theoretical Analysis

MedKoo Cat#: 573171

Name: CH7057288

CAS#: 2095616-82-1

Chemical Formula: C32H31N3O5S

Exact Mass: 569.1984

Molecular Weight: 569.68

Elemental Analysis: C, 67.47; H, 5.49; N, 7.38; O, 14.04; S, 5.63

Price and Availability

Size	Price	Availability
1mg	USD 80.00	Ready to ship
5mg	USD 150.00	Ready to ship
10mg	USD 250.00	Ready to ship
25mg	USD 450.00	Ready to ship
50mg	USD 750.00	Ready to ship
100mg	USD 1,350.00	Ready to ship
200mg	USD 2,350.00	Ready to ship

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Related CAS #

No Data

Synonym

CH7057288; CH-7057288; CH 7057288;

IUPAC/Chemical Name

N-(tert-butyl)-2-((6,6-dimethyl-8-(methylsulfonamido)-11-oxo-6,11-dihydronaphtho[2,3-b]benzofuran-3-yl)ethynyl)-6-methylisonicotinamide

InChi Key

DCGOHGQJHJXBGW-UHFFFAOYSA-N

InChi Code

InChI=1S/C32H31N3O5S/c1-18-14-20(30(37)34-31(2,3)4)16-21(33-18)10-8-19-9-12-24-26(15-19)40-29-27(24)28(36)23-13-11-22(35-41(7,38)39)17-25(23)32(29,5)6/h9,11-17,35H,1-7H3,(H,34,37)

SMILES Code

CS(NC1=CC=C2C(C(C)(C)C(OC3=CC(C#CC4=NC(C)=CC(C(NC(C)(C)C)=O)=C4)=CC=C35)=C5C2=O)=C1)(=O)=O

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

Shelf Life

>3 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

2934.99.03.00

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#C22R03B18

QC Data

View QC data: current batch, Lot#C22R03B18

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

CH7057288 is a potent and selective TRK inhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively.

In vitro activity:

CH7057288’s cellular inhibition of TRK activity was investigated using three TRK fusion–positive cancer cell lines. CH7057288 potently inhibited autophosphorylation of TRK in a dose-dependent manner. As for downstream signaling of TRK fusion, phosphorylation of the PLCγ1, MAPK, and Akt pathways were investigated, since these three pathways are known to be involved in TRK. CH7057288 suppressed phosphorylation of PLCγ1 and ERK, although suppression levels varied somewhat in different cell lines, and Akt phosphorylation was slightly inhibited in CUTO-3 but strongly suppressed in KM12-Luc and MO-91. These observations indicate that CH7057288 has inhibitory activity to TRK and blocks TRK fusion–mediated signaling in cells. Reference: Mol Cancer Ther. 2018 Dec;17(12):2519-2529. https://pubmed.ncbi.nlm.nih.gov/30242093/

In vivo activity:

CH7057288 was tested in an intracranial implantation model of CUTO-3-Luc that mimics metastasis to the central nervous system (CNS). Luminescence was reduced after CH7057288 treatment but was enhanced in the vehicle control group, indicating regression of intracranial tumors by the compound. When event-free survival was assessed, survival was significantly prolonged by 30-day CH7057288 treatment compared with vehicle treatment. The CH7057288-treated animals survived throughout the treatment without events, in contrast to the control mice, of which more than half were removed from the experiment by Day 26. Mean survival of the treated group reached 67 days after treatment initiation. These tests collectively show that CH7057288 demonstrated potent in vivo antitumor activity, with reasonable pharmacodynamic response in subcutaneous xenograft models and prolonged event-free survival in an intracranial model. Reference: Mol Cancer Ther. 2018 Dec;17(12):2519-2529. https://pubmed.ncbi.nlm.nih.gov/30242093/

	Solvent	mg/mL	mM
Solubility
	DMSO	34.0	59.68

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 569.68 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. Tanaka H, Sase H, Tsukaguchi T, Hasegawa M, Tanimura H, Yoshida M, Sakata K, Fujii T, Tachibana Y, Takanashi K, Higashida A, Hasegawa K, Ono Y, Oikawa N, Mio T. Selective TRK Inhibitor CH7057288 against TRK Fusion-Driven Cancer. Mol Cancer Ther. 2018 Dec;17(12):2519-2529. doi: 10.1158/1535-7163.MCT-17-1180. Epub 2018 Sep 21. PMID: 30242093.

In vitro protocol:

In vivo protocol:

1: Tanaka H, Sase H, Tsukaguchi T, Hasegawa M, Tanimura H, Yoshida M, Sakata K, Fujii T, Tachibana Y, Takanashi K, Higashida A, Hasegawa K, Ono Y, Oikawa N, Mio T. Selective TRK inhibitor CH7057288 against TRK fusion-driven cancer. Mol Cancer Ther. 2018 Sep 21. pii: molcanther.1180.2017. doi: 10.1158/1535-7163.MCT-17-1180. [Epub ahead of print] PubMed PMID: 30242093.