BS-181 HCl
- CAS NO.:1397219-81-6
- Empirical Formula: C22H33ClN6
- Molecular Weight: 416.99062
- MDL number: MFCD18384975
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:03
What is BS-181 HCl?
Biological Activity
normal progression through the cell cycle requires the sequential action of cyclin-dependent kinases cdk1, cdk2, cdk4, and cdk6. direct or indirect deregulation of cdk activity is a feature of almost all cancers and has led to the development of cdk inhibitors as anticancer agents.bs-181 is a highly selective cdk7 inhibitor with ic50 of 21 nm. ; >40-fold selective for cdk7 than cdk1, 2, 4, 5, 6, or 9.
in vitro
bs-181, inhibited cak activity with an ic50 of 21 nmol/l. testing of other cdks as well as another 69 kinases showed that bs-181 only inhibited cdk2 at concentrations lower than 1 μmol/l, with cdk2 being inhibited 35-fold less potently (ic50 880 nmol/l) than cdk7. in mcf-7 cells, bs-181 inhibited the phosphorylation of cdk7 substrates, promoted cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines [1].
in vivo
bs-181 was stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. the same dose of drug inhibited the growth of mcf-7 human xenografts in nude mice. bs-181 therefore provides the first example of a potent and selective cdk7 inhibitor with potential as an anticancer agent [1].
References
[1] ali s, heathcote da, kroll sh, jogalekar as, scheiper b, patel h, brackow j, siwicka a, fuchter mj, periyasamy m, tolhurst rs, kanneganti sk, snyder jp, liotta dc, aboagye eo, barrett ag, coombes rc. the development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. cancer res. 2009;69(15):6208-15.
Properties of BS-181 HCl
storage temp. | under inert gas (nitrogen or Argon) at 2–8 °C |
solubility | insoluble in H2O; ≥20.85 mg/mL in DMSO; ≥6.49 mg/mL in EtOH with ultrasonic |
form | solid |
color | White to off-white |
Safety information for BS-181 HCl
Signal word | Danger |
Pictogram(s) |
Flame Flammables GHS02 Corrosion Corrosives GHS05 |
GHS Hazard Statements |
H226:Flammable liquids H314:Skin corrosion/irritation |
Precautionary Statement Codes |
P210:Keep away from heat/sparks/open flames/hot surfaces. — No smoking. P233:Keep container tightly closed. P240:Ground/bond container and receiving equipment. P241:Use explosion-proof electrical/ventilating/lighting/…/equipment. P242:Use only non-sparking tools. P243:Take precautionary measures against static discharge. P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P280:Wear protective gloves/protective clothing/eye protection/face protection. P363:Wash contaminated clothing before reuse. P301+P330+P331:IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. P303+P361+P353:IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. P370+P378:In case of fire: Use … for extinction. P405:Store locked up. P403+P235:Store in a well-ventilated place. Keep cool. |
Computed Descriptors for BS-181 HCl
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