CBPD-409

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MedKoo CAT#: 126625

CAS#: N/A

Description: CBPD-409 is a highly potent, selective, and orally bioavailable CBP/p300 degrader. CBPD-409 induces robust CBP/p300 degradation with DC50 0.2−0.4 nM and displays strong antiproliferative effects with IC50 1.2−2.0 nM in the VCaP, LNCaP, and 22Rv1 AR+ prostate cancer cell lines. It has a favorable pharmacokinetic profile and achieves 50% of oral bioavailability in mice. A single oral administration of CBPD-409 at 1 mg/kg achieves >95% depletion of CBP/p300 proteins in the VCaP tumor tissue. CBPD-409 exhibits strong tumor growth inhibition and is much more potent and efficacious than two CBP/p300 inhibitors CCS1477 and GNE-049 and the AR antagonist Enzalutamide.

Chemical Structure

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CBPD-409
CAS# N/A
Instruction

Theoretical Analysis

MedKoo Cat#: 126625
Name: CBPD-409
CAS#: N/A
Chemical Formula: C46H52F2N10O5
Exact Mass: 862.41
Molecular Weight: 862.984
Elemental Analysis: C, 64.02; H, 6.07; F, 4.40; N, 16.23; O, 9.27

Price and Availability

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 @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: CBPD-409; CBPD409; CBPD 409

IUPAC/Chemical Name: 5-(4-((4-(5-acetyl-3-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)cyclohexyl)methyl)piperazin-1-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

InChi Key: CXJGNQXWKVPWMM-MNKVZQORSA-N

InChi Code: InChI=1S/C46H52F2N10O5/c1-27(59)55-15-13-38-37(26-55)43(56-14-3-4-29-20-34(30-23-49-52(2)25-30)35(42(47)48)22-40(29)56)51-58(38)31-7-5-28(6-8-31)24-53-16-18-54(19-17-53)32-9-10-33-36(21-32)46(63)57(45(33)62)39-11-12-41(60)50-44(39)61/h9-10,20-23,25,28,31,39,42H,3-8,11-19,24,26H2,1-2H3,(H,50,60,61)/t28-,31?,39?

SMILES Code: CN1N=CC(C2=CC3=C(N(C4=NN(C5=C4CN(C(C)=O)CC5)C6CC[C@H](CN7CCN(C8=CC=C9C(C(N(C%10C(NC(CC%10)=O)=O)C9=O)=O)=C8)CC7)CC6)CCC3)C=C2C(F)F)=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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 862.98 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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Chen Z, Wang M, Wu D, Zhao L, Metwally H, Jiang W, Wang Y, Bai L, McEachern D, Luo J, Wang M, Li Q, Matvekas A, Wen B, Sun D, Chinnaiyan AM, Wang S. Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer. J Med Chem. 2024 Mar 26. doi: 10.1021/acs.jmedchem.3c01789. Epub ahead of print. PMID: 38530938.