MedKoo Cat#: 122399 | Name: WK500B
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

WK500B is a BCL6 inhibitor. WK500B engaged BCL6 inside cells, blocked BCL6 repression complexes, reactivated BCL6 target genes, killed DLBCL cells and caused apoptosis as well as cell cycle arrest. In animal models, WK500B inhibited germinal center (GC) formation and DLBCL tumour growth without toxic and side effects. Moreover, WK500B displayed strong efficacy and favourable pharmacokinetics and presented superior druggability.

Chemical Structure

WK500B
WK500B
CAS#2253985-29-2

Theoretical Analysis

MedKoo Cat#: 122399

Name: WK500B

CAS#: 2253985-29-2

Chemical Formula: C22H23BrFN7O

Exact Mass: 499.1131

Molecular Weight: 500.38

Elemental Analysis: C, 52.81; H, 4.63; Br, 15.97; F, 3.80; N, 19.60; O, 3.20

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to Ship
10mg USD 250.00 Ready to Ship
25mg USD 550.00 Ready to Ship
50mg USD 950.00 Ready to Ship
100mg USD 1,650.00 Ready to Ship
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Related CAS #
No Data
Synonym
WK500B; WK 500B; WK-500B
IUPAC/Chemical Name
6-bromo-N-(4-((2-((3S,5R)-3,5-dimethylpiperazin-1-yl)-5-fluoropyrimidin-4-yl)amino)phenyl)picolinamide
InChi Key
YJGYJPZYSQTACG-OKILXGFUSA-N
InChi Code
InChI=1S/C22H23BrFN7O/c1-13-11-31(12-14(2)26-13)22-25-10-17(24)20(30-22)27-15-6-8-16(9-7-15)28-21(32)18-4-3-5-19(23)29-18/h3-10,13-14,26H,11-12H2,1-2H3,(H,28,32)(H,25,27,30)/t13-,14+
SMILES Code
C[C@H](N[C@H](C)C1)CN1C2=NC(NC(C=C3)=CC=C3NC(C4=CC=CC(Br)=N4)=O)=C(F)C=N2
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
WK500B is a BCL6 inhibitor.
In vitro activity:
To be determined
In vivo activity:
WK500B is a promising candidate that could be developed as an effective orally available therapeutic agent for diffuse large B cell lymphoma (DLBCL). In animal models, WK500B inhibited germinal center (GC) formation and DLBCL tumour growth without toxic and side effects. WK500B displayed strong efficacy and favourable pharmacokinetics and presented superior druggability. Reference: Cancer Lett. 2022 Mar 31;529:100-111. https://pubmed.ncbi.nlm.nih.gov/34990752/

Preparing Stock Solutions

The following data is based on the product molecular weight 500.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Xing Y, Guo W, Wu M, Xie J, Huang D, Hu P, Zhou M, Zhang L, Zhang Q, Wang P, Wang X, Wang G, Wu H, Zhou C, Chen Y, Liu M, Yi Z, Sun Z. An orally available small molecule BCL6 inhibitor effectively suppresses diffuse large B cell lymphoma cells growth in vitro and in vivo. Cancer Lett. 2022 Mar 31;529:100-111. doi: 10.1016/j.canlet.2021.12.035. Epub 2022 Jan 4. PMID: 34990752.
In vitro protocol:
To be determined
In vivo protocol:
1. Xing Y, Guo W, Wu M, Xie J, Huang D, Hu P, Zhou M, Zhang L, Zhang Q, Wang P, Wang X, Wang G, Wu H, Zhou C, Chen Y, Liu M, Yi Z, Sun Z. An orally available small molecule BCL6 inhibitor effectively suppresses diffuse large B cell lymphoma cells growth in vitro and in vivo. Cancer Lett. 2022 Mar 31;529:100-111. doi: 10.1016/j.canlet.2021.12.035. Epub 2022 Jan 4. PMID: 34990752.
Xing Y, Guo W, Wu M, Xie J, Huang D, Hu P, Zhou M, Zhang L, Zhang Q, Wang P, Wang X, Wang G, Wu H, Zhou C, Chen Y, Liu M, Yi Z, Sun Z. An orally available small molecule BCL6 inhibitor effectively suppresses diffuse large B cell lymphoma cells growth in vitro and in vivo. Cancer Lett. 2022 Mar 31;529:100-111. doi: 10.1016/j.canlet.2021.12.035. Epub 2022 Jan 4. PMID: 34990752.