BMS 214662
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Grundinformationen
- CAS
195987-41-8- Standard-SMILES
N#Cc1ccc2c(c1)CN(S(=O)(=O)c1cccs1)[C@H](Cc1ccccc1)CN2Cc1cnc[nH]1- InChIKey
OLCWFLWEHWLBTO-HSZRJFAPSA-N- Summenformel
- C25H23N5O2S2
- Durchschnittliche Molmasse
- 489,626 g/mol
- Monoisotopische Masse
- 489,12931698
Namen und Bezeichner
- Bevorzugter Name
- BMS 214662
- IUPAC
- (3R)-3-Benzyl-1-[(1H-imidazol-5-yl)methyl]-4-(thiophene-2-sulfonyl)-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-carbonitrile
- Englischer Name
- (4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile
- Summenformel
- C25H23N5O2S2
- Molmasse
- 489.62
Namen und Synonyme
BMS214662BMS 2146627-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine(R)-2,3,4,5-Tetrahydro-1-(1H-iMidazol-4-ylMethyl)-3-(phenylMethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-ca(4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile(3R)-2,3,4,5-Tetrahydro-1-(1H-iMidazol-4-ylMethyl)-3-(phenylMethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile(3R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-5-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile(3R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-5-ylmethyl)-3-(benzyl)-4-(thiophen-2-ylsulfonyl)-1H-benzo[e][1,4]diazepin-7-carbonitrile1H-1,4-Benzodiazepine-7-carbonitrile,2,3,4,5-tetrahydro-1-(1H-iMidazol-5-ylMethyl)-3-(phenylMethyl)-4-(2-thienylsulfonyl)-,(3R)-
Datenbank-Bezeichner
- CAS
195987-41-8- PubChem CID
Eigenschaften
Physikochemische Eigenschaften
- Siedepunkt
- 790.9 · 790.9±70.0 °C(Predicted)
- Dichte
- 1.45 · 1.45±0.1 g/cm3(Predicted)
- storage temp.
- -20 °C · Store at -20°C
- Löslichkeit
- DMSO: slightly soluble; Methanol: slightly soluble
- Aggregatzustand
- A solid
- pka
- 13.19 · 13.19±0.10(Predicted)
- Farbe
- White to off-white
Chemie und Industrie
Anwendungen
BeschreibungBMS 214662 is a potent inhibitor of farnesyltransferase (FTase; IC50 = 1.3 nM). It is selective for FTase over geranylgeranyl transferase (GGTase; IC50 = 1,900 nM). It inhibits the growth of MEK2, A2780, and PC3 cancer cells expressing wild-type Ras (IC50s = 2.5, 0.04, and 0.15 μM, respectively), as well as HCT116, MIP, RC-165, and MIA PaCa-2 cells expressing mutant K-Ras (IC50s = 0.06, 0.3, 0.3, and 0.12 μM, respectively). BMS 214662 induces apoptosis in HCT116 cells in a concentration-dependent manner. In vivo, BMS 214662 (600 mg/kg) is curative in an HCT116 mouse xenograft model. It also reduces tumor growth in Calu-1, HT-29, EJ-1, and MIA PaCa-2 mouse xenograft models.
VerwendenA potent and selective inhibitor of farnesyltransferase that induces mitochondrial apoptosis in chronic myeloid leukemia stem/progenitor cells, including CD34+38- cells, through activation of protein kinase Cβ.
Anbieter34 Anbieter
成都超九八生物科技有限公司13348960310 13348960310 · [email protected]
United Life Science020-82099279 18988968278 · [email protected]
InvivoChem中国13549236410 · [email protected]
砌块化学科技（上海）有限公司021-20432219 13918097649 · [email protected]
銳迪國際科技有限公司18024082417 · [email protected]
MedChemexpress LLC021-58955995 · [email protected]
上海尺水药物研究有限公司[email protected] 13564957716 · [email protected]
凯试（上海）科技有限公司021-50135380 · [email protected]
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