MedKoo Cat#: 128288 | Name: QZ2135

Description:

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

QZ2135 is a RET PROTAC Degrader with Enhanced Antiproliferative Activity against Resistant Cancer Cells Harboring RET Solvent-Front Mutations. QZ2135 effectively degraded RET kinase and its resistant mutants, such as V804M and G810C/R. It also exhibited superior antiproliferative activity against Ba/F3cells stably expressing oncogenic fusions of RET with solvent-front mutants, including G810C/R/S, compared to its parental inhibitor. Notably, QZ2135 demonstrated in vivo antitumor efficacy in a Ba/F3-KIF5B-RET-G810C xenograft mouse model.

Chemical Structure

QZ2135
QZ2135
CAS#N/A

Theoretical Analysis

MedKoo Cat#: 128288

Name: QZ2135

CAS#: N/A

Chemical Formula: C53H54N12O4

Exact Mass: 922.4391

Molecular Weight: 923.10

Elemental Analysis: C, 68.96; H, 5.90; N, 18.21; O, 6.93

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 #
No Data
Synonym
QZ2135; QZ 2135; QZ-2135
IUPAC/Chemical Name
6-(1-(1-(7-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)hept-6-yn-1-yl)piperidin-4-yl)-1H-pyrazol-4-yl)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile
InChi Key
IQGZDJDFIILZLB-UHFFFAOYSA-N
InChi Code
InChI=1S/C53H54N12O4/c1-69-50-16-11-35(25-56-50)29-62-42-23-43(62)33-61(32-42)48-14-12-37(26-55-48)45-22-38(30-65-51(45)39(24-54)27-58-65)40-28-57-64(31-40)41-17-20-60(21-18-41)19-6-4-2-3-5-8-36-9-7-10-44-46(36)34-63(53(44)68)47-13-15-49(66)59-52(47)67/h7,9-12,14,16,22,25-28,30-31,41-43,47H,2-4,6,13,15,17-21,23,29,32-34H2,1H3,(H,59,66,67)
SMILES Code
N#CC1=C2C(C3=CC=C(N4CC(C5)N(CC6=CC=C(OC)N=C6)C5C4)N=C3)=CC(C7=CN(C8CCN(CCCCCC#CC9=CC=CC%10=C9CN(C(CC%11)C(NC%11=O)=O)C%10=O)CC8)N=C7)=CN2N=C1
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 923.10 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
Zhang Q, He Y, Rao D, He R, Yu L, Sun Y, Lai Y, Shi Z, Peng L, Zhang Z, Xu S. Discovery of an Efficacious RET PROTAC Degrader with Enhanced Antiproliferative Activity against Resistant Cancer Cells Harboring RET Solvent-Front Mutations. J Med Chem. 2024 Dec 28. doi: 10.1021/acs.jmedchem.4c02692. Epub ahead of print. PMID: 39731581.