CH7233163


Catalog No. Size PriceQuantity
M16733-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S.

Product information

Molecular Weight: 669.72

Formula: C31H34F3N9O3S

Chemical Name: N-[2-(1-cyclopropylsulfonylpyrazol-4-yl)pyrimidin-4-yl]-7-(4-methylpiperazin-1-yl)-5-propan-2-yl-9-(2, 2, 2-trifluoroethoxy)pyrido[4, 3-b]indol-3-amine

Smiles: CN1CCN(CC1)C1=CC2=C(C(=C1)OCC(F)(F)F)C1=CN=C(C=C1N2C(C)C)NC1=CC=NC(=N1)C1C=NN(C=1)S(=O)(=O)C1CC1

InChiKey: KMBMYNDPNVGEFI-UHFFFAOYSA-N

InChi: InChI=1S/C31H34F3N9O3S/c1-19(2)43-24-14-28(38-27-6-7-35-30(39-27)20-15-37-42(17-20)47(44,45)22-4-5-22)36-16-23(24)29-25(43)12-21(41-10-8-40(3)9-11-41)13-26(29)46-18-31(32,33)34/h6-7,12-17,19,22H,4-5,8-11,18H2,1-3H3,(H,35,36,38,39)

Technical Data

Appearance: Solid Power

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

Solubility: Solubility (25°C). DMSO: 100 mg/mL(149.31 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

CH7233163 shows potent antitumor activities against tumor with EGFR-Del19/T790M/C797S in vitro. CH7233163 potently inhibits the proliferation of Del19/T790M/C797S_NIH3T3 cells with IC50 of 20 nmol/L. CH7233163 potently and dose-dependently blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 can inhibit Del19/T790M/C797S signaling.

In Vivo:

Pharmacodynamic study is performed using Del19/T790M/C797S_NIH3T3 xenografted tumors in mice. CH7233163 clearly inhibits EGFR phosphorylation after oral administration and potent tumor regression is observed. CH7233163 has potent therapeutic efficacy against tumors with EGFR-Del19/T790M/C797S in vivo.

Products are for research use only. Not for human use.

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