CH7057288
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MedKoo CAT#: 573171

CAS#: 2095616-82-1

Description: 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

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CH7057288
CAS# 2095616-82-1
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 573171
Name: CH7057288
CAS#: 2095616-82-1
Chemical Formula: C32H31N3O5S
Exact Mass: 569.20
Molecular Weight: 569.680
Elemental Analysis: C, 67.47; H, 5.49; N, 7.38; O, 14.04; S, 5.63

Price and Availability

Size Price Availability Quantity
1mg USD 80 Ready to ship
5mg USD 150 Ready to ship
10mg USD 250 Ready to ship
25mg USD 450 Ready to ship
50mg USD 750 Ready to ship
100mg USD 1350 Ready to ship
200mg USD 2350 Ready to ship
Bulk inquiry

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:

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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 34.0 59.68

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.

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. 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: 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 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 Dec;17(12):2519-2529. doi: 10.1158/1535-7163.MCT-17-1180. Epub 2018 Sep 21. PMID: 30242093.

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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.