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MedKoo Cat#: 333107 | Name: Sotuletinib 2HCl
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Description:

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

Sotuletinib, also known as 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.

Chemical Structure

Sotuletinib 2HCl
Sotuletinib 2HCl
CAS#2222138-40-9 (2HCl)

Theoretical Analysis

MedKoo Cat#: 333107

Name: Sotuletinib 2HCl

CAS#: 2222138-40-9 (2HCl)

Chemical Formula: C20H24Cl2N4O3S

Exact Mass: 0.0000

Molecular Weight: 471.40

Elemental Analysis: C, 50.96; H, 5.13; Cl, 15.04; N, 11.89; O, 10.18; S, 6.80

Price and Availability

Size Price Availability Quantity
25mg USD 150.00 2 Weeks
50mg USD 250.00 2 Weeks
100mg USD 450.00 2 Weeks
200mg USD 750.00 2 Weeks
500mg USD 1,650.00 2 Weeks
1g USD 2,950.00 2 Weeks
2g USD 5,250.00 2 Weeks
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Related CAS #
2222138-40-9 (2HCl) 2222138-31-8 (HCl) 953769-46-5 (free base)
Synonym
Sotuletinib 2HCl; BLZ945; BLZ 945; BLZ-945; Sotuletinib dihydrochloride
IUPAC/Chemical Name
4-((2-(((1R,2R)-2-hydroxycyclohexyl)amino)benzo[d]thiazol-6-yl)oxy)-N-methylpicolinamide dihydrochloride
InChi Key
ZIHWHYXECXSBNA-LVVRIOTCSA-N
InChi Code
InChI=1S/C20H22N4O3S.2ClH/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);2*1H/t14-,17-;;/m1../s1
SMILES Code
O=C(NC)C1=NC=CC(OC2=CC=C3N=C(N[C@H]4[C@H](O)CCCC4)SC3=C2)=C1.[H]Cl.[H]Cl
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

Preparing Stock Solutions

The following data is based on the product molecular weight 471.40 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
1: Zheng C, Zhong Q, Yi K, Kong H, Cao F, Zhuo C, Xu Y, Shi R, Ju E, Song W, Tao Y, Chen X, Li M. Anti-phagocytosis-blocking repolarization-resistant membrane- fusogenic liposome (ARMFUL) for adoptive cell immunotherapy. Sci Adv. 2023 Aug 9;9(32):eadh2413. doi: 10.1126/sciadv.adh2413. Epub 2023 Aug 9. PMID: 37556535; PMCID: PMC10411906. 2: Dye CN, Franceschelli D, Leuner B, Lenz KM. Microglia depletion facilitates the display of maternal behavior and alters activation of the maternal brain network in nulliparous female rats. Neuropsychopharmacology. 2023 Jun 17. doi: 10.1038/s41386-023-01624-1. Epub ahead of print. PMID: 37330580. 3: Huang Y, Yang C, Lv J, Zhang Y, Wang K, Ma L, Liu Z, Yu H, Li M, Tang Z. Formula optimization and in vivo study of poly(L-glutamic acid)-g-methoxy poly(ethylene glycol)/combretastatin A4/BLZ945 nanoparticles for cancer therapy. Int J Pharm. 2023 Apr 5;636:122849. doi: 10.1016/j.ijpharm.2023.122849. Epub 2023 Mar 17. PMID: 36933582. 4: An X, Wang J, Tong L, Zhang X, Fu H, Zhang J, Xie H, Huang Y, Jia H. 18F-Labeled o‑aminopyridyl alkynyl radioligands targeting colony- stimulating factor 1 receptor for neuroinflammation imaging. Bioorg Med Chem. 2023 Apr 1;83:117233. doi: 10.1016/j.bmc.2023.117233. Epub 2023 Mar 8. PMID: 36933438. 5: Thongchot S, Duangkaew S, Yotchai W, Maungsomboon S, Phimolsarnti R, Asavamongkolkul A, Thuwajit P, Thuwajit C, Chandhanayingyong C. Novel CSF1R-positive tenosynovial giant cell tumor cell lines and their pexidartinib (PLX3397) and sotuletinib (BLZ945)-induced apoptosis. Hum Cell. 2023 Jan;36(1):456-467. doi: 10.1007/s13577-022-00823-0. Epub 2022 Dec 2. PMID: 36456782; PMCID: PMC9813176. 6: Kesarwani P, Kant S, Zhao Y, Miller CR, Chinnaiyan P. The Influence of the Ketogenic Diet on the Immune Tolerant Microenvironment in Glioblastoma. Cancers (Basel). 2022 Nov 11;14(22):5550. doi: 10.3390/cancers14225550. PMID: 36428642; PMCID: PMC9688691. 7: Pognan F, Buono C, Couttet P, Galarneau JR, Timsit Y, Wolf A. Liver enzyme delayed clearance in rat treated by CSF1 receptor specific antagonist Sotuletinib. Curr Res Toxicol. 2022 Oct 29;3:100091. doi: 10.1016/j.crtox.2022.100091. PMID: 36353522; PMCID: PMC9637862. 8: Chokr SM, Milinkeviciute G, Jimenez GA, Abubakr H, Cramer KS. Long-term microglia depletion impairs synapse elimination and auditory brainstem function. Sci Rep. 2022 Nov 2;12(1):18521. doi: 10.1038/s41598-022-23250-5. PMID: 36323869; PMCID: PMC9630367. 9: Xie X, Feng Y, Zhang H, Su Q, Song T, Yang G, Li N, Wei X, Li T, Qin X, Li S, Wu C, Zhang X, Wang G, Liu Y, Yang H. Remodeling tumor immunosuppressive microenvironment via a novel bioactive nanovaccines potentiates the efficacy of cancer immunotherapy. Bioact Mater. 2022 Mar 11;16:107-119. doi: 10.1016/j.bioactmat.2022.03.008. Erratum in: Bioact Mater. 2022 Sep 07;21:239-240. PMID: 35386322; PMCID: PMC8958467. 10: Hwang D, Seyedsadr MS, Ishikawa LLW, Boehm A, Sahin Z, Casella G, Jang S, Gonzalez MV, Garifallou JP, Hakonarson H, Zhang W, Xiao D, Rostami A, Zhang GX, Ciric B. CSF-1 maintains pathogenic but not homeostatic myeloid cells in the central nervous system during autoimmune neuroinflammation. Proc Natl Acad Sci U S A. 2022 Apr 5;119(14):e2111804119. doi: 10.1073/pnas.2111804119. Epub 2022 Mar 30. PMID: 35353625; PMCID: PMC9168454. 11: Kosti CN, Vaitsi PC, Pappas AG, Iliopoulou MP, Psarra KK, Magkouta SF, Kalomenidis IT. CSF1/CSF1R signaling mediates malignant pleural effusion formation. JCI Insight. 2022 Mar 22;7(6):e155300. doi: 10.1172/jci.insight.155300. PMID: 35315360; PMCID: PMC8986064. 12: Klemm F, Möckl A, Salamero-Boix A, Alekseeva T, Schäffer A, Schulz M, Niesel K, Maas RR, Groth M, Elie BT, Bowman RL, Hegi ME, Daniel RT, Zeiner PS, Zinke J, Harter PN, Plate KH, Joyce JA, Sevenich L. Compensatory CSF2-driven macrophage activation promotes adaptive resistance to CSF1R inhibition in breast-to-brain metastasis. Nat Cancer. 2021 Oct;2(10):1086-1101. doi: 10.1038/s43018-021-00254-0. Epub 2021 Oct 18. PMID: 35121879. 13: Borse V, Kaur T, Hinton A, Ohlemiller K, Warchol ME. Programmed Cell Death Recruits Macrophages Into the Developing Mouse Cochlea. Front Cell Dev Biol. 2021 Dec 9;9:777836. doi: 10.3389/fcell.2021.777836. PMID: 34957108; PMCID: PMC8696258. 14: Wies Mancini VSB, Di Pietro AA, de Olmos S, Silva Pinto P, Vence M, Marder M, Igaz LM, Marcora MS, Pasquini JM, Correale JD, Pasquini LA. Colony- stimulating factor-1 receptor inhibition attenuates microgliosis and myelin loss but exacerbates neurodegeneration in the chronic cuprizone model. J Neurochem. 2022 Mar;160(6):643-661. doi: 10.1111/jnc.15566. Epub 2022 Jan 9. PMID: 34935149. 15: Sun X, Zhang J, Zhao X, Yang C, Shi M, Zhang B, Hu H, Qiao M, Chen D, Zhao X. Binary regulation of the tumor microenvironment by a pH-responsive reversible shielding nanoplatform for improved tumor chemo-immunotherapy. Acta Biomater. 2022 Jan 15;138:505-517. doi: 10.1016/j.actbio.2021.11.017. Epub 2021 Nov 16. PMID: 34798317. 16: Pfirschke C, Zilionis R, Engblom C, Messemaker M, Zou AE, Rickelt S, Gort- Freitas NA, Lin Y, Bill R, Siwicki M, Gungabeesoon J, Sprachman MM, Marquard AN, Rodell CB, Cuccarese MF, Quintana J, Ahmed MS, Kohler RH, Savova V, Weissleder R, Klein AM, Pittet MJ. Macrophage-Targeted Therapy Unlocks Antitumoral Cross- talk between IFNγ-Secreting Lymphocytes and IL12-Producing Dendritic Cells. Cancer Immunol Res. 2022 Jan;10(1):40-55. doi: 10.1158/2326-6066.CIR-21-0326. Epub 2021 Dec 1. PMID: 34795032; PMCID: PMC10132467. 17: van der Wildt B, Miao Z, Reyes ST, Park JH, Klockow JL, Zhao N, Romero A, Guo SG, Shen B, Windhorst AD, Chin FT. BLZ945 derivatives for PET imaging of colony stimulating factor-1 receptors in the brain. Nucl Med Biol. 2021 Sep- Oct;100-101:44-51. doi: 10.1016/j.nucmedbio.2021.06.005. Epub 2021 Jun 23. PMID: 34174546. 18: Fang Y, He Y, Wu C, Zhang M, Gu Z, Zhang J, Liu E, Xu Q, Asrorov AM, Huang Y. Magnetism-mediated targeting hyperthermia-immunotherapy in "cold" tumor with CSF1R inhibitor. Theranostics. 2021 May 3;11(14):6860-6872. doi: 10.7150/thno.57511. PMID: 34093858; PMCID: PMC8171105. 19: Magkouta SF, Vaitsi PC, Pappas AG, Iliopoulou M, Kosti CN, Psarra K, Kalomenidis IT. CSF1/CSF1R Axis Blockade Limits Mesothelioma and Enhances Efficiency of Anti-PDL1 Immunotherapy. Cancers (Basel). 2021 May 22;13(11):2546. doi: 10.3390/cancers13112546. PMID: 34067348; PMCID: PMC8196870. 20: Liaw K, Reddy R, Sharma A, Li J, Chang M, Sharma R, Salazar S, Kannan S, Kannan RM. Targeted systemic dendrimer delivery of CSF-1R inhibitor to tumor- associated macrophages improves outcomes in orthotopic glioblastoma. Bioeng Transl Med. 2020 Dec 11;6(2):e10205. doi: 10.1002/btm2.10205. PMID: 34027092; PMCID: PMC8126814.

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BGB-16673

BGB-16673

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