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BI-2493

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BI-2493 Basic information

Product Name:
BI-2493
Synonyms:
  • Spiro[1,2-benzisoxazole-7(4H),4′(5′H)-benzo[b]thiophene]-3′-carbonitrile, 2′-amino-5,6,6′,7′-tetrahydro-3-[2-[(2S)-2-methyl-1-piperazinyl]-4-pyrimidinyl]-, (4′S)-
  • bi-2493
  • (S)-2-Amino-3'-(2-((S)-2-methylpiperazin-1-yl)pyrimidin-4-yl)-5',6,6',7-tetrahydro-4'H,5H-spiro[benzo[b]thiophene-4,7'-benzo[d]isoxazole]-3-carbonitrile
  • (S)-2-Amino-3'-[2-[(S)-2-methyl-1-piperazinyl]-4-pyrimidinyl]-5',6,6',7-tetrahydro-4'H,5H-spiro[benzo[b]thiophene-4,7'-benzo[d]isoxazole]-3-carbonitrile
  • (S)-2-Amino-3'-(2-((S)-2-methylpiperazin-1-yl)pyrimidin-4-yl)-5',6,6',7-tetrahydro-4'H,5H-spiro[benzo[b]thiophene-4,7'-benzo[d]isoxazole]-3-carbonitrile
CAS:
2937344-16-4
MF:
C24H27N7OS
MW:
461.58
Mol File:
2937344-16-4.mol
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BI-2493 Chemical Properties

Boiling point:
774.2±70.0 °C(Predicted)
Density 
1.41±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)
pka
8.62±0.40(Predicted)
form 
Solid
color 
Off-white to light yellow
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BI-2493 Usage And Synthesis

Uses

BI-2493 is a structural analog of BI-2865 and a highly selective pan-KRAS inhibitor. This compound can attenuate tumor growth and can also be used for cancer disease research.

in vivo

BI-2493 (90 mg/kg, p.o., twice daily for 21 days) exhibits tumor-suppressive activity in LS513/GP2d/HPAC/SW620/MIAPACA2-derived xenograft NMRI mice models[1].

Animal Model:LS513/GP2d/HPAC/SW620/MIAPACA2-derived xenograft NMRI mice models
Dosage:90 mg/kg
Administration:Oral gavage (p.o.), twice daily for 21 days
Result:Reduced tumor growth in mice carrying KRAS G12C, G12D, G12V, and A146V mutation models, without causing significant toxicity to the mice.

IC 50

K-Ras WT

BI-2493Supplier

Shanghai Tachizaki Biomedical Research Center Gold
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BOC Sciences
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Shanghai Topbiochem Technology Co., Ltd
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ShangHai Caerulum Pharma Discovery Co., Ltd.
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Hangzhou J&H Chemical Co., Ltd.
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