BGB324 (R428)
featured

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

MedKoo CAT#: 401810

CAS#: 1037624-75-1

Description: BGB-324, also known as R428 or Bemcentinib, is a selective small molecule inhibitor of Axl kinase, which showed activity to blocks tumor spread and prolongs survival in models of metastatic breast cancer. The receptor tyrosine kinase Axl may play an important role in cancer progression, invasion, metastasis, drug resistance, and patient mortality. R428 inhibits Axl with low nanomolar activity and blocked Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production.


Price and Availability

Size
Price

25mg
USD 150
200mg
USD 850
2g
USD 5250
Size
Price

50mg
USD 250
500mg
USD 1850
5g
USD 9950
Size
Price

100mg
USD 450
1g
USD 3250

BGB324 (R428) purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 401810
Name: BGB324 (R428)
CAS#: 1037624-75-1
Chemical Formula: C30H34N8
Exact Mass: 506.29064
Molecular Weight: 506.64
Elemental Analysis: C, 71.12; H, 6.76; N, 22.12


Synonym: BGB324; BGB-324; BGB 324; R 428; R-428; R428; Bemcentinib

IUPAC/Chemical Name: (S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine

InChi Key: KXMZDGSRSGHMMK-VWLOTQADSA-N

InChi Code: InChI=1S/C30H34N8/c31-29-33-30(32-24-13-10-20-11-14-25(15-12-22(20)18-24)37-16-3-4-17-37)36-38(29)27-19-23-8-5-7-21-6-1-2-9-26(21)28(23)35-34-27/h1-2,6,9-10,13,18-19,25H,3-5,7-8,11-12,14-17H2,(H3,31,32,33,36)/t25-/m0/s1

SMILES Code: NC1=NC(NC2=CC=C3C(CC[C@@H](N4CCCC4)CC3)=C2)=NN1C5=NN=C6C(CCCC7=CC=CC=C76)=C5


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (MSDS):

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).

Harmonized System Code:
2934.99.90.01


Additional Information

  
 
 
 


References

1: Sadahiro H, Kang KD, Gibson JT, Minata M, Yu H, Shi J, Chhipa RR, Chen Z, Lu S, Simoni Y, Furuta T, Sabit H, Zhang S, Bastola S, Yamaguchi S, Alsheikh HA, Komarova S, Wang J, Kim SH, Hambardzumyan D, Lu X, Newell EW, Dasgupta B, Nakada M, Lee LJ, Nabors LB, Norian LA, Nakano I. Activation of the receptor tyrosine kinase AXL regulates the immune microenvironment in glioblastoma. Cancer Res. 2018 Mar 12. pii: canres.2433.2017. doi: 10.1158/0008-5472.CAN-17-2433. [Epub ahead of print] PubMed PMID: 29531161.

2: Oien DB, Garay T, Eckstein S, Chien J. Cisplatin and Pemetrexed Activate AXL and AXL Inhibitor BGB324 Enhances Mesothelioma Cell Death from Chemotherapy. Front Pharmacol. 2018 Jan 11;8:970. doi: 10.3389/fphar.2017.00970. eCollection 2017. PubMed PMID: 29375377; PubMed Central PMCID: PMC5768913.

3: Ludwig KF, Du W, Sorrelle NB, Wnuk-Lipinska K, Topalovski M, Toombs JE, Cruz VH, Yabuuchi S, Rajeshkumar NV, Maitra A, Lorens JB, Brekken RA. Small-Molecule Inhibition of Axl Targets Tumor Immune Suppression and Enhances Chemotherapy in Pancreatic Cancer. Cancer Res. 2018 Jan 1;78(1):246-255. doi: 10.1158/0008-5472.CAN-17-1973. Epub 2017 Nov 27. PubMed PMID: 29180468; PubMed Central PMCID: PMC5754222.

4: Palisoul ML, Quinn JM, Schepers E, Hagemann IS, Guo L, Reger K, Hagemann AR, McCourt CK, Thaker PH, Powell MA, Mutch DG, Fuh KC. Inhibition of the Receptor Tyrosine Kinase AXL Restores Paclitaxel Chemosensitivity in Uterine Serous Cancer. Mol Cancer Ther. 2017 Dec;16(12):2881-2891. doi: 10.1158/1535-7163.MCT-17-0587. Epub 2017 Sep 13. PubMed PMID: 28904132; PubMed Central PMCID: PMC5716844.

5: Young CS, Clarke KM, Kettyle LM, Thompson A, Mills KI. Decitabine-Vorinostat combination treatment in acute myeloid leukemia activates pathways with potential for novel triple therapy. Oncotarget. 2017 May 19;8(31):51429-51446. doi: 10.18632/oncotarget.18009. eCollection 2017 Aug 1. PubMed PMID: 28881658; PubMed Central PMCID: PMC5584259.

6: Hong Q, Li O, Zheng W, Xiao WZ, Zhang L, Wu D, Cai GY, He JC, Chen XM. LncRNA HOTAIR regulates HIF-1α/AXL signaling through inhibition of miR-217 in renal cell carcinoma. Cell Death Dis. 2017 May 11;8(5):e2772. doi: 10.1038/cddis.2017.181. PubMed PMID: 28492542; PubMed Central PMCID: PMC5520706.

7: Lin JZ, Wang ZJ, De W, Zheng M, Xu WZ, Wu HF, Armstrong A, Zhu JG. Targeting AXL overcomes resistance to docetaxel therapy in advanced prostate cancer. Oncotarget. 2017 Jun 20;8(25):41064-41077. doi: 10.18632/oncotarget.17026. PubMed PMID: 28455956; PubMed Central PMCID: PMC5522277.

8: von Mässenhausen A, Brägelmann J, Billig H, Thewes B, Queisser A, Vogel W, Kristiansen G, Schröck A, Bootz F, Brossart P, Kirfel J, Perner S. Implication of the Receptor Tyrosine Kinase AXL in Head and Neck Cancer Progression. Int J Mol Sci. 2016 Dec 22;18(1). pii: E7. doi: 10.3390/ijms18010007. PubMed PMID: 28025482; PubMed Central PMCID: PMC5297642.

9: Ben-Batalla I, Erdmann R, Jørgensen H, Mitchell R, Ernst T, von Amsberg G, Schafhausen P, Velthaus JL, Rankin S, Clark RE, Koschmieder S, Schultze A, Mitra S, Vandenberghe P, Brümmendorf TH, Carmeliet P, Hochhaus A, Pantel K, Bokemeyer C, Helgason GV, Holyoake TL, Loges S. Axl Blockade by BGB324 Inhibits BCR-ABL Tyrosine Kinase Inhibitor-Sensitive and -Resistant Chronic Myeloid Leukemia. Clin Cancer Res. 2017 May 1;23(9):2289-2300. doi: 10.1158/1078-0432.CCR-16-1930. Epub 2016 Nov 17. PubMed PMID: 27856601.

10: Dowall SD, Bewley K, Watson RJ, Vasan SS, Ghosh C, Konai MM, Gausdal G, Lorens JB, Long J, Barclay W, Garcia-Dorival I, Hiscox J, Bosworth A, Taylor I, Easterbrook L, Pitman J, Summers S, Chan-Pensley J, Funnell S, Vipond J, Charlton S, Haldar J, Hewson R, Carroll MW. Antiviral Screening of Multiple Compounds against Ebola Virus. Viruses. 2016 Oct 27;8(11). pii: E277. PubMed PMID: 27801778; PubMed Central PMCID: PMC5127007.

11: Antony J, Tan TZ, Kelly Z, Low J, Choolani M, Recchi C, Gabra H, Thiery JP, Huang RY. The GAS6-AXL signaling network is a mesenchymal (Mes) molecular subtype-specific therapeutic target for ovarian cancer. Sci Signal. 2016 Oct 4;9(448):ra97. PubMed PMID: 27703030.

12: Tong LS, Shao AW, Ou YB, Guo ZN, Manaenko A, Dixon BJ, Tang J, Lou M, Zhang JH. Recombinant Gas6 augments Axl and facilitates immune restoration in an intracerebral hemorrhage mouse model. J Cereb Blood Flow Metab. 2017 Jun;37(6):1971-1981. doi: 10.1177/0271678X16658490. Epub 2016 Jan 1. PubMed PMID: 27389179; PubMed Central PMCID: PMC5464693.

13: Wang C, Jin H, Wang N, Fan S, Wang Y, Zhang Y, Wei L, Tao X, Gu D, Zhao F, Fang J, Yao M, Qin W. Gas6/Axl Axis Contributes to Chemoresistance and Metastasis in Breast Cancer through Akt/GSK-3β/β-catenin Signaling. Theranostics. 2016 May 24;6(8):1205-19. doi: 10.7150/thno.15083. eCollection 2016. PubMed PMID: 27279912; PubMed Central PMCID: PMC4893646.

14: Del Pozo Martin Y, Park D, Ramachandran A, Ombrato L, Calvo F, Chakravarty P, Spencer-Dene B, Derzsi S, Hill CS, Sahai E, Malanchi I. Mesenchymal Cancer Cell-Stroma Crosstalk Promotes Niche Activation, Epithelial Reversion, and Metastatic Colonization. Cell Rep. 2015 Dec 22;13(11):2456-2469. doi: 10.1016/j.celrep.2015.11.025. Epub 2015 Dec 6. PubMed PMID: 26670048; PubMed Central PMCID: PMC4695340.

15: Ocal O, Pashkov V, Kollipara RK, Zolghadri Y, Cruz VH, Hale MA, Heath BR, Artyukhin AB, Christie AL, Tsoulfas P, Lorens JB, Swift GH, Brekken RA, Wilkie TM. A rapid in vivo screen for pancreatic ductal adenocarcinoma therapeutics. Dis Model Mech. 2015 Oct 1;8(10):1201-11. doi: 10.1242/dmm.020933. PubMed PMID: 26438693; PubMed Central PMCID: PMC4610235.

16: Bansal N, Mishra PJ, Stein M, DiPaola RS, Bertino JR. Axl receptor tyrosine kinase is up-regulated in metformin resistant prostate cancer cells. Oncotarget. 2015 Jun 20;6(17):15321-31. PubMed PMID: 26036314; PubMed Central PMCID: PMC4558154.

17: Vouri M, An Q, Birt M, Pilkington GJ, Hafizi S. Small molecule inhibition of Axl receptor tyrosine kinase potently suppresses multiple malignant properties of glioma cells. Oncotarget. 2015 Jun 30;6(18):16183-97. PubMed PMID: 25980499; PubMed Central PMCID: PMC4599264.

18: Bárcena C, Stefanovic M, Tutusaus A, Joannas L, Menéndez A, García-Ruiz C, Sancho-Bru P, Marí M, Caballeria J, Rothlin CV, Fernández-Checa JC, de Frutos PG, Morales A. Gas6/Axl pathway is activated in chronic liver disease and its targeting reduces fibrosis via hepatic stellate cell inactivation. J Hepatol. 2015 Sep;63(3):670-8. doi: 10.1016/j.jhep.2015.04.013. Epub 2015 Apr 20. PubMed PMID: 25908269; PubMed Central PMCID: PMC4543529.

19: Brand TM, Iida M, Stein AP, Corrigan KL, Braverman CM, Coan JP, Pearson HE, Bahrar H, Fowler TL, Bednarz BP, Saha S, Yang D, Gill PS, Lingen MW, Saloura V, Villaflor VM, Salgia R, Kimple RJ, Wheeler DL. AXL Is a Logical Molecular Target in Head and Neck Squamous Cell Carcinoma. Clin Cancer Res. 2015 Jun 1;21(11):2601-12. doi: 10.1158/1078-0432.CCR-14-2648. Epub 2015 Mar 12. PubMed PMID: 25767293; PubMed Central PMCID: PMC5032632.

20: Jin CW, Wang H, Chen YQ, Tang MX, Fan GQ, Wang ZH, Li L, Zhang Y, Zhang W, Zhong M. Gas6 delays senescence in vascular smooth muscle cells through the PI3K/ Akt/FoxO signaling pathway. Cell Physiol Biochem. 2015;35(3):1151-66. doi: 10.1159/000373940. Epub 2015 Feb 6. PubMed PMID: 25766527.