Brigimadlin HCl | CAS#2095116-40-6 | MDM2 inhibitor

MedKoo Cat#: 123387 | Name: Brigimadlin HCl

Description:

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

Brigimadlin, also known as BI-907828, is an E3 ubiquitin-protein ligase Mdm2 inhibitor with potential as an antineoplastic agent.BI-907828 is a novel potent MDM2 inhibitor. BI-907828 inhibits GBM brain tumor stem cells in vitro and prolongs survival in orthotopic xenograft mouse models. BI-907828 decreases viability and induces cell death at picomolar concentrations, in both MDM2 amplified and normal copy number, TP53 wild-type BTSC lines. BI-907828 provides a promising new therapeutic option for patients with TP53 wild-type primary brain tumors.

Chemical Structure

Brigimadlin HCl

CAS#Brigimadlin HCl

Theoretical Analysis

MedKoo Cat#: 123387

Name: Brigimadlin HCl

CAS#: Brigimadlin HCl

Chemical Formula: C31H26Cl3FN4O3

Exact Mass: 590.1300

Molecular Weight: 627.92

Elemental Analysis: C, 59.30; H, 4.17; Cl, 16.94; F, 3.03; N, 8.92; O, 7.64

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

2095116-40-6 (free base) Brigimadlin HCl

Synonym

Brigimadlin HCl; BI 907828; BI-907828; BI907828; GTPL12627;

IUPAC/Chemical Name

(3S,3'S,3a'R,10a'R)-6-chloro-3'-(3-chloro-2-fluorophenyl)-1'-(cyclopropylmethyl)-6'-methyl-2-oxo-3',3a',10',10a'-tetrahydro-1'H-spiro[indoline-3,2'-pyrrolo[2',3':4,5]pyrrolo[1,2-b]indazole]-7'-carboxylic acid hydrochloride

InChi Key

MOYXEZWJGHFHJD-ZNGUJEIKSA-N

InChi Code

InChI=1S/C31H25Cl2FN4O3.ClH/c1-14-17(29(39)40)8-9-18-23-12-24-28(38(23)36-27(14)18)25(19-3-2-4-21(33)26(19)34)31(37(24)13-15-5-6-15)20-10-7-16(32)11-22(20)35-30(31)41;/h2-4,7-11,15,24-25,28H,5-6,12-13H2,1H3,(H,35,41)(H,39,40);1H/t24-,25+,28+,31-;/m1./s1

SMILES Code

O=C(C1=C(C)C2=NN3C(C[C@](N4CC5CC5)([H])[C@@]3([H])[C@H](C6=CC=CC(Cl)=C6F)[C@@]74C(NC8=C7C=CC(Cl)=C8)=O)=C2C=C1)O.[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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 627.92 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: Konopleva M, Martinelli G, Daver N, Papayannidis C, Wei A, Higgins B, Ott M, Mascarenhas J, Andreeff M. MDM2 inhibition: an important step forward in cancer therapy. Leukemia. 2020 Nov;34(11):2858-2874. doi: 10.1038/s41375-020-0949-z. Epub 2020 Jul 10. PMID: 32651541. 2: Hao X, Bahia R, Cseh O, Bozek D, Blake S, Rinnenthal J, Weyer-Czernilofsky U, Rudolph D, Luchman HA. BI-907828, a novel potent MDM2 inhibitor, inhibits GBM brain tumor stem cells in vitro and prolongs survival in orthotopic xenograft mouse models. Neuro Oncol. 2022 Dec 15:noac271. doi: 10.1093/neuonc/noac271. Epub ahead of print. PMID: 36521007. 3: Cornillie J, Wozniak A, Li H, Gebreyohannes YK, Wellens J, Hompes D, Debiec- Rychter M, Sciot R, Schöffski P. Anti-tumor activity of the MDM2-TP53 inhibitor BI-907828 in dedifferentiated liposarcoma patient-derived xenograft models harboring MDM2 amplification. Clin Transl Oncol. 2020 Apr;22(4):546-554. doi: 10.1007/s12094-019-02158-z. Epub 2019 Jun 14. PMID: 31201607. 4: Schöffski P, Lahmar M, Lucarelli A, Maki RG. Brightline-1: phase II/III trial of the MDM2-p53 antagonist BI 907828 versus doxorubicin in patients with advanced DDLPS. Future Oncol. 2023 Mar 29. doi: 10.2217/fon-2022-1291. Epub ahead of print. PMID: 36987836. 5: Glimmers of Hope for Targeting p53. Cancer Discov. 2022 Aug 5;12(8):OF5. doi: 10.1158/2159-8290.CD-ND2022-0009. PMID: 35686841.