BX-912A potent and selective PDK-1 inhibitor that induces apoptosis

BX-912 (CAS 702674-56-4)

BX-912 | CAS 702674-56-4 is rated 5.0 out of 5 by 1.
  • y_2019, m_11, d_19, h_13
  • bvseo_bulk, prod_bvrr, vn_bulk_3.0.3-b1
  • cp_1, bvpage1
  • co_hasreviews, tv_0, tr_1
  • loc_en_US, sid_364451, prod, sort_[SortEntry(order=SUBMISSION_TIME, direction=DESCENDING)]
  • clientName_scbt
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getAggregateRating, 177ms
  • REVIEWS, PRODUCT
5
1
4
0
3
0
2
0
1
0
Synonym: N-(3-(4-(2-(1H-imidazol-5-yl)ethylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide
Application: A potent and selective PDK-1 inhibitor that induces apoptosis
CAS Number: 702674-56-4
Purity: ≥97%
Molecular Weight: 471.35
Molecular Formula: C20H23BrN8O
* Refer to Certificate of Analysis for lot specific data (including water content).
Submit a review for this product and receive 15 CruzCredits

BX-912 is a 3-Phosphoinositide-dependent Kinase-1 (PDK-1) inhibitor. BX 912 suppresses growth in a number of cell lines and also induces apoptosis. Cell lines with elevated levels of AKT are >30-fold more sensitive to PDK1 inhibition by BX-912. This compound is a competitive inhibitor of PDK1, indicating that it binds to the ATP-binding pocket to inhibit phosphorylation. BX-912 accomplishes this due to the fact that the aminopyrimidine backbone, which adopts a similar conformation to ATP in the active site of PDK1. BX-912 potently inhibits the growth of PC-3 cells in soft agar, displaying an IC50 of 320 nM.


References

1. Feldman RI, et al. J Biol Chem. 2005, 280(20), 19867-19874.

Appearance :
Powder
Physical State :
Solid
Storage :
Store at -20° C
Melting Point :
305.47° C (Predicted)
Boiling Point :
698.81° C (Predicted)
Density :
~1.6 g/cm3 (Predicted)
Refractive Index :
n20D 1.75 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11754511
SMILES :
C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCC4=CN=CN4)Br

Download SDS (MSDS)

Certificate of Analysis

Adobe Acrobat Reader is required to reliably view,
print and comment on PDF documents

BX-912  Product Citations

See how others have used BX-912. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 25736282  Yu, ZL. et al. 2015. Journal of cardiovascular pharmacology and therapeutics. 20: 563-71.

Citations 1 to 1 of 1 total

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. BX-912, sc-364451, is in off-white powder form.
Answered by: Chemical Support 4
Date published: 2017-05-22

What is the solubility of this chemical?

Asked by: two2igm05
Thank you for your question. BX-912, sc-364451, is soluble in DMSO at 94 mg/mL (199 mM), in Water at <1 mg/mL (<1 mM), and in Ethanol at 94 mg/mL (199 mM).
Answered by: TechService7
Date published: 2016-12-15
  • y_2019, m_11, d_19, h_13CST
  • bvseo_bulk, prod_bvqa, vn_bulk_3.0.3-b1
  • cp_1, bvpage1
  • co_hasquestionsanswers, tq_2
  • loc_en_US, sid_364451, prod, sort_[SortEntry(order=LAST_APPROVED_ANSWER_SUBMISSION_TIME, direction=DESCENDING)]
  • clientName_scbt
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getContent, 162ms
  • QUESTIONS, PRODUCT
Rated 5 out of 5 by from Sturm et al Sturm et al. (PubMed ID 25645675) used BX-912 to inhibit PDK1 while studying PDK1's inhibitory effects on eosinophillic inflammation. -SCBT Publication Review
Date published: 2015-07-15
  • y_2019, m_11, d_19, h_13
  • bvseo_bulk, prod_bvrr, vn_bulk_3.0.3-b1
  • cp_1, bvpage1
  • co_hasreviews, tv_0, tr_1
  • loc_en_US, sid_364451, prod, sort_[SortEntry(order=SUBMISSION_TIME, direction=DESCENDING)]
  • clientName_scbt
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getReviews, 27ms
  • REVIEWS, PRODUCT

Santa Cruz Biotechnology, Inc. is a world leader in the development of products for the biomedical research market. Call us Toll Free at 1-800-457-3801.
Copyright © 2007-2019 Santa Cruz Biotechnology, Inc. All Rights Reserved. "Santa Cruz Biotechnology", and the Santa Cruz Biotechnology, Inc. logo, "Santa Cruz Animal Health", "San Juan Ranch", "Supplement of Champions", the San Juan Ranch logo, "Ultracruz", "Chemcruz", "Immunocruz", "Exactacruz", and "EZ Touch" are registered trademarks of Santa Cruz Biotechnology, Inc.
All trademarks are the property of their respective owners.