WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407110
CAS#: 953769-46-5
Description: BLZ945 is a potent and selective CSF-1R kinase inhibitor. BLZ945 showed effects of CSF1R inhibition on other tumor-infiltrating immune cells. BLZ945 attenuates the turnover rate of TAMs while increasing the number of CD8+ T cells that infiltrate cervical and breast carcinomas. BLZ945 decreases the growth of malignant cells in the mouse mammary tumor virus-driven polyomavirus middle T antigen (MMTV-PyMT) model of mammary carcinogenesis. BLZ945 prevents tumor progression in the keratin 14-expressing human papillomavirus type 16 (K14-HPV-16) transgenic model of cervical carcinogenesis.
MedKoo Cat#: 407110
Name: BLZ945
CAS#: 953769-46-5
Chemical Formula: C20H22N4O3S
Exact Mass: 398.14126
Molecular Weight: 398.48
Elemental Analysis: C, 60.28; H, 5.57; N, 14.06; O, 12.04; S, 8.05
Synonym: BLZ945; BLZ 945; BLZ-945.
IUPAC/Chemical Name: 4-((2-(((1R,2R)-2-hydroxycyclohexyl)amino)benzo[d]thiazol-6-yl)oxy)-N-methylpicolinamide
InChi Key: ADZBMFGQQWPHMJ-RHSMWYFYSA-N
InChi Code: InChI=1S/C20H22N4O3S/c1-21-19(26)16-10-13(8-9-22-16)27-12-6-7-15-18(11-12)28-20(24-15)23-14-4-2-3-5-17(14)25/h6-11,14,17,25H,2-5H2,1H3,(H,21,26)(H,23,24)/t14-,17-/m1/s1
SMILES Code: O=C(NC)C1=NC=CC(OC2=CC3=C(N=C(N[C@@H]4CCCC[C@H]4O)S3)C=C2)=C1
Appearance: Solid powder
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: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
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
The following data is based on the product molecular weight 398.48 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.
| 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 |
1: Krauser JA, Jin Y, Walles M, Pfaar U, Sutton J, Wiesmann M, Graf D, Pflimlin-Fritschy V, Wolf T, Camenisch G, Swart P. Phenotypic and metabolic investigation of a CSF-1R kinase receptor inhibitor (BLZ945) and its pharmacologically active metabolite. Xenobiotica. 2015 Feb;45(2):107-23. doi: 10.3109/00498254.2014.945988. Epub 2014 Sep 2. PubMed PMID: 25180976.
2: Bowman RL, Joyce JA. Therapeutic targeting of tumor-associated macrophages and microglia in glioblastoma. Immunotherapy. 2014;6(6):663-6. doi: 10.2217/imt.14.48. PubMed PMID: 25041027.
3: Strachan DC, Ruffell B, Oei Y, Bissell MJ, Coussens LM, Pryer N, Daniel D. CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8(+) T cells. Oncoimmunology. 2013 Dec 1;2(12):e26968. Epub 2013 Dec 4. PubMed PMID: 24498562; PubMed Central PMCID: PMC3902121.
4: Wang T, Papoutsi M, Wiesmann M, DeCristofaro M, Keselica MC, Skuba E, Spaet R, Markovits J, Wolf A, Moulin P, Pognan F, Vancutsem P, Petryk L, Sutton J, Chibout SD, Kluwe W. Investigation of correlation among safety biomarkers in serum, histopathological examination, and toxicogenomics. Int J Toxicol. 2011 May;30(3):300-12. doi: 10.1177/1091581811401920. Epub 2011 Jun 8. PubMed PMID: 21653914.
