WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H123387
CAS#: Brigimadlin HCl
Description: 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.
Hodoodo Cat#: H123387
Name: Brigimadlin HCl
CAS#: Brigimadlin HCl
Chemical Formula: C31H25Cl2FN4O3
Exact Mass: 590.13
Molecular Weight: 591.460
Elemental Analysis: C, 62.95; H, 4.26; Cl, 11.99; F, 3.21; N, 9.47; O, 8.11
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.
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
InChi Key: AMTXDBGKYPDTTA-UOHKKRDWSA-N
InChi Code: InChI=1S/C31H25Cl2FN4O3/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)/t24-,25+,28+,31-/m1/s1
SMILES Code: CC1=C(C(O)=O)C=CC2=C(C[C@@]([H])(N(CC3CC3)[C@]4(C5=CC=C(Cl)C=C5NC4=O)[C@H]6C7=C(F)C(Cl)=CC=C7)[C@]86[H])N8N=C21
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: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 591.46 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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
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.