MedKoo Cat#: 463244 | Name: CG428
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Description:

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

CG428 is a tropomyosin receptor kinase (TRK) degrader that targets the intracellular kinase domain of TRK. CG428 reduced levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells and inhibited downstream PLCγ1 signaling at sub-nanomolar concentrations. CG428 also degraded human wild-type TRKA.

Chemical Structure

CG428
CG428
CAS#2412055-93-5

Theoretical Analysis

MedKoo Cat#: 463244

Name: CG428

CAS#: 2412055-93-5

Chemical Formula: C43H43FN10O6

Exact Mass: 814.3351

Molecular Weight: 814.88

Elemental Analysis: C, 63.38; H, 5.32; F, 2.33; N, 17.19; O, 11.78

Price and Availability

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5mg USD 750.00 2 Weeks
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Related CAS #
No Data
Synonym
CG428; CG 428; CG-428;
IUPAC/Chemical Name
2-(2,6-dioxopiperidin-3-yl)-4-((2-(3-(4-(6-(6-((R)-2-(3-fluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazin-3-yl)pyridin-2-yl)piperazin-1-yl)-3-oxopropoxy)ethyl)amino)isoindoline-1,3-dione
InChi Key
FWANKJAOTQAHHR-KWRHIPAJSA-N
InChi Code
InChI=1S/C43H43FN10O6/c44-28-6-1-5-27(25-28)32-10-4-18-52(32)37-14-13-35-46-26-34(54(35)49-37)30-8-3-11-36(47-30)50-19-21-51(22-20-50)39(56)16-23-60-24-17-45-31-9-2-7-29-40(31)43(59)53(42(29)58)33-12-15-38(55)48-41(33)57/h1-3,5-9,11,13-14,25-26,32-33,45H,4,10,12,15-24H2,(H,48,55,57)/t32-,33?/m1/s1
SMILES Code
O=C(CC1)NC(C1N(C2=O)C(C3=C2C(NCCOCCC(N(CC4)CCN4C5=NC(C6=CN=C(C=C7)N6N=C7N8CCC[C@@H]8C9=CC=CC(F)=C9)=CC=C5)=O)=CC=C3)=O)=O
Appearance
Solid powder
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
Soluble in DMSO
Shelf Life
>3 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).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 814.88 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
1: Chen L, Chen Y, Zhang C, Jiao B, Liang S, Tan Q, Chai H, Yu W, Qian Y, Yang H, Yao W, Yu J, Luo Y, Plewe M, Wang J, Han XR, Liu J. Discovery of First-In- Class Potent and Selective Tropomyosin Receptor Kinase Degraders. J Med Chem. 2020 Oct 15. doi: 10.1021/acs.jmedchem.0c01342. Epub ahead of print. PMID: 33058680.