Free shipping on all orders over $ 500

BS-181

Cat. No. M13598
BS-181 Structure
Size Price Availability
5mg USD 110  USD110 4-7 Days
10mg USD 180  USD180 4-7 Days
50mg USD 610  USD610 4-7 Days
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

BS-181 is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib . BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy.

Chemical Information
Molecular Weight 380.53
CAS Number 1092443-52-1
Solubility (25°C) DMSO ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hangzhan Ma, et al. Ther Adv Musculoskelet Dis. Cyclin-dependent kinase 7 (CDK7) is an emerging prognostic biomarker and therapeutic target in osteosarcoma

[2] Shin Young Park, et al. Cancers (Basel). G 1 Cell Cycle Arrest and Extrinsic Apoptotic Mechanisms Underlying the Anti-Leukemic Activity of CDK7 Inhibitor BS-181

[3] Honghai Hong, et al. J Cell Mol Med. CDK7 inhibition suppresses rheumatoid arthritis inflammation via blockage of NF-κB activation and IL-1β/IL-6 secretion

[4] Bo-Yong Wang, et al. Drug Des Devel Ther. Selective CDK7 inhibition with BS-181 suppresses cell proliferation and induces cell cycle arrest and apoptosis in gastric cancer

[5] Yong Xia, et al. Clin Exp Med. Selective inhibition of CDK7 ameliorates experimental arthritis in mice

Related CDK Products
PF-07224826

PF-07224826 is a CDK2/4/6 inhibitor.

INCB123667

INCB123667 is a CDK2 inhibitor.

Senexin B

Senexin B is a potent, orally active CDK8/19 inhibitor with Kd values of 140 nM and 80 nM for CDK8 and CDK19, respectively.

Q901

Q901 is a CDK7 inhibitor for tumor-related studies.

NUV-422

NUV-422 is a CDK2/4/6 inhibitor that can be used in studies related to malignant gliomas.

  Catalog
Abmole Inhibitor Catalog




Keywords: BS-181 supplier, CDK, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.