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Cat. No.: HY-161498

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XYD198

XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC₅₀ of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia.
(Pink: CBP/p300 ligand (HY-161495); Blue: Cereblon ligand (HY-41547); Black: linker (HY-161499)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

화학식: C₅₄H₄₉F₂N₁₁O₇
분자량:1002.03

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

XYD198 Chemical Structure

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC₅₀ of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia^[1]. (Pink: CBP/p300 ligand (HY-161495); Blue: Cereblon ligand (HY-41547); Black: linker (HY-161499)).

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

All Histone Acetyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	IC₅₀	47 nM Compound: 14h; XYD198	Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by Cell-Titer Glo assay Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by Cell-Titer Glo assay	[PMID: 38649304]
MOLM-16	IC₅₀	5.5 nM Compound: 14h; XYD198	Antiproliferative activity against human MOLM16 cells incubated for 72 hrs by Cell-Titer Glo assay Antiproliferative activity against human MOLM16 cells incubated for 72 hrs by Cell-Titer Glo assay	[PMID: 38649304]
MV4-11	IC₅₀	0.9 nM Compound: 14h; XYD198	Antiproliferative activity against human MV4-11 cells incubated for 120 hrs by Cell-Titer Glo assay Antiproliferative activity against human MV4-11 cells incubated for 120 hrs by Cell-Titer Glo assay	[PMID: 38649304]

In Vitro

XYD198 (0-1 μM, 72-120 h) inhibits proliferations of acute myeloid leukemia (AML) cells MV4;11, MOLM-13 and MOLM-16, with the IC₅₀ of 0.9, 47 and 5.5 nM, respectively^[1].
XYD198 (0-150 nM, 6 h) induces CBP and p300 degradation in bromodomain family proteins in a CRBN- and proteasome-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

MV4;11 AML, MOLM-13 and MOLM-16
Concentration:

0-1 μM
Incubation Time:

3 days for MOLM-13, 4 days for MV4;11 AML and MOLM-16
Result:

Inhibited cell proliferation.

Western Blot Analysis^[1]

Cell Line:

MV4;11 AML, MOLM-13 and MOLM-16
Concentration:

0-150 nM
Incubation Time:

6 h
Result:

Degraded CBP and p300 proteins.

In Vivo

CBP/p300 ligand 4 (5 mg/kg, p.o., every other day for 2 weeks) exhibits antitumor activity in MV4;11 xenograft mice model, with a tumor growth inhibition rate TGI of 93%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

MV4;11 xenograft NOD-SCID mice model^[1]
Dosage:

5 mg/kg
Administration:

p.o., every other day for 2 weeks
Result:

Inhibited tumor growth with a TGI of 93%.

Chemical Information

분자량 1002.03
화학식 C₅₄H₄₉F₂N₁₁O₇
SMILES

O=C1CCC[C@H](N1C2=CC=C(C(F)=C2)F)C3=NC4=C(C=CC(C5=C(ON=C5C)C)=C4)N3C6CCN(CC6)CC(NC7=CN=C(N=C7)C8=CC=C(C=C8)CNC9=CC=CC(C(N%10C%11C(NC(CC%11)=O)=O)=O)=C9C%10=O)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Hu J, et al., Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity. J Med Chem. 2024 May 9;67(9):6952-6986. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

XYD198

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms

All Histone Acetyltransferase Isoforms