BS-181 HCl Property

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

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H226Flammable liquid and vapour

H314Causes severe skin burns and eye damage

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P233Keep container tightly closed.

P240Ground/bond container and receiving equipment.

P241Use explosion-proof electrical/ventilating/lighting/…/equipment.

P242Use only non-sparking tools.

P243Take precautionary measures against static discharge.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P330+P331IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.

P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.

P363Wash contaminated clothing before reuse.

P370+P378In case of fire: Use … for extinction.

P403+P235Store in a well-ventilated place. Keep cool.

P405Store locked up.

BS-181 HCl Chemical Properties,Usage,Production

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].

target

CDK7

IC 50

21 nm (cdk7)

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.