TAS2940

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MedKoo CAT#: 130142

CAS#: N/A

Description: TAS2940 is an irreversible pan-ERBB inhibitor with increased brain penetrability for treatment of lung cancers where metastasis has occurred in the brain, as well as glioblastomas, with HER2/EGFR exon 20 insertions and EGFR aberrations. TAS2940 was shown to be effective and increased survival rate of mice in intracranial xenograft models of HER2/EGFR cancers. TAS2940 is currently undergoing phase 1 clinical trials for solid tumors to determine maximum tolerable dosage.


Chemical Structure

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TAS2940
CAS# N/A

Theoretical Analysis

MedKoo Cat#: 130142
Name: TAS2940
CAS#: N/A
Chemical Formula: C28H30N6O2
Exact Mass: 482.24
Molecular Weight: 482.590
Elemental Analysis: C, 69.69; H, 6.27; N, 17.41; O, 6.63

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: TAS2940

IUPAC/Chemical Name: 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N-((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide

InChi Key: KJWHUTTYFUQYBW-WAOWUJCRSA-N

InChi Code: InChI=1S/C28H30N6O2/c1-4-23(35)33-15-21(14-17(33)2)34-22(13-12-19-10-11-19)24(25-26(29)30-16-31-27(25)34)28(36)32-18(3)20-8-6-5-7-9-20/h4-9,16-19,21H,1,10-11,14-15H2,2-3H3,(H,32,36)(H2,29,30,31)/t17-,18+,21+/m0/s1

SMILES Code: O=C(C1=C(C#CC2CC2)N([C@H]3CN(C(C=C)=O)[C@@H](C)C3)C4=NC=NC(N)=C41)N[C@@H](C5=CC=CC=C5)C

Appearance: To be determined

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 482.59 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:
In vitro protocol:
In vivo protocol:

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1. Oguchi K, Araki H, Tsuji S, Nakamura M, Miura A, Funabashi K, Osada A, Tanaka S, Suzuki T, Kobayashi SS, Mizuarai S. TAS2940, a novel brain-penetrable pan-ERBB inhibitor, for tumors with HER2 and EGFR aberrations. Cancer Sci. 2023 Feb;114(2):654-664. doi: 10.1111/cas.15617. Epub 2022 Nov 13. PMID: 36282234; PMCID: PMC9899605.

2. https://clinicaltrials.gov/ct2/show/NCT04982926