2758034-98-7

Name	7H-Pyrrolo[2,3-d]pyrimidine-5-carboxamide, 4-amino-6-(2-cyclopropylethynyl)-7-[(3R,5S)-5-methyl-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]-N-[(1R)-1-phenylethyl]-, (2E)-2-butenedioate (1:1)
CAS	2758034-98-7
Molecular Formula	C28H30N6O2.C4H4O4
Molecular Weight	598.65
MOL File	2758034-98-7.mol

Synonyms

7H-Pyrrolo[2,3-d]pyrimidine-5-carboxamide, 4-amino-6-(2-cyclopropylethynyl)-7-[(3R,5S)-5-methyl-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]-N-[(1R)-1-phenylethyl]-, (2E)-2-butenedioate (1:1)

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Hazard Information

Uses

TAS2940 fumarate is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 fumarate against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 fumarate can be used for the study of tumors with HER2 and EGFR aberrations[1].

in vivo

TAS2940 fumarate (3.1-25 mg/kg; po; once daily; for 14?days) inhibits tumor growth in xenograft mouse models with ERBB aberrations: HER2 amplification, HER2/EGFR exon 20 insertions, and EGFR vIII mutation^[1].
PK parameters of TAS2940 after a single oral administration or multiple oral administrations for 7 days in male BALB/cAJcl-nu/nu mice^[1].

1.19

Administration	Dose (mg/kg)	T_max (h)	Apparent T_1/2 (h)	C_max (ng/mL)	AUC_last (ng?h/mL)
Single administration	6.25	0.33±0.14	2.15±2.15	601±111	795±229
Single administration	12.5	0.25±0.00	NC	1590±220	2010±230
Single administration	25	0.25±0.00	2.09	3580±190	5080±820
Repeated administrations for 7 days	6.25	0.25±0.00	2.20±2.73	1170±300	972±239
Repeated administrations for 7 days	12.5	0.33±0.14	0.69	2040±230	2800±460
Repeated administrations for 7 days	25	0.42±0.14	0.76	3710±360	6180±310

Animal Model:	6-week-old male BALB/cAJcl-nu/nu mice injected with NCI-N87, MCF10A_HER2/insYVMA_v, or NCI-H1975 EGFR D770_N771insSVD cellsMCF10A_HER2/insYVMA_v^[1]
Dosage:	3.1-25 mg/kg (0.5 w/v% HPMC)
Administration:	po; once daily; for 14?days
Result:	Inhibited tumor growth in xenograft mouse models.

References

[1] Kei Oguchi, et al. 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

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Websitehttps://www.targetmol.cn/

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