WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H123192
CAS#: N/A
Description: CPD-1224 is heterobifunctional degrader (proteolysis targeting chimeras, PROTAC). CPD-1224 avoided hemolysis (a feature of detergent-like PROTACs), degraded the otherwise recalcitrant mutant L1196M/G1202R in vivo, and commensurately slowed tumor growth, while the third generation ALK inhibitor drug lorlatinib had no effect.
Hodoodo Cat#: H123192
Name: CPD-1224
CAS#: N/A
Chemical Formula: C43H47ClN8O7S
Exact Mass: 854.30
Molecular Weight: 855.410
Elemental Analysis: C, 60.38; H, 5.54; Cl, 4.14; N, 13.10; O, 13.09; S, 3.75
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Synonym: CPD-1224; CPD1224; CPD 1224
IUPAC/Chemical Name: 5-(3-((4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-methoxy-2-methylphenyl)piperidin-1-yl)methyl)azetidin-1-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
InChi Key: YROLXKJYDUJWRK-UHFFFAOYSA-N
InChi Code: InChI=1S/C43H47ClN8O7S/c1-24(2)60(57,58)37-8-6-5-7-33(37)46-39-32(44)20-45-43(49-39)47-34-17-25(3)30(19-36(34)59-4)27-13-15-50(16-14-27)21-26-22-51(23-26)28-9-10-29-31(18-28)42(56)52(41(29)55)35-11-12-38(53)48-40(35)54/h5-10,17-20,24,26-27,35H,11-16,21-23H2,1-4H3,(H,48,53,54)(H2,45,46,47,49)
SMILES Code: ClC(C=NC(NC1=CC(C)=C(C2CCN(CC3CN(C4=CC(C(N(C5C(NC(CC5)=O)=O)C6=O)=O)=C6C=C4)C3)CC2)C=C1OC)=N7)=C7NC8=C(S(C(C)C)(=O)=O)C=CC=C8
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 855.41 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: |
Gao Y, Jiang B, Kim H, Berberich MJ, Che J, Donovan KA, Hatcher JM, Huerta F, Kwiatkowski NP, Liu Y, Liuni PP, Metivier RJ, Murali VK, Nowak RP, Zhang T, Fischer ES, Gray NS, Jones LH. Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions. J Med Chem. 2023 Apr 10. doi: 10.1021/acs.jmedchem.2c01864. Epub ahead of print. PMID: 37036171.