NX-2127

Name: NX-2127
Brand: MedChemExpress
SKU: HY-153220
Rating: 4.5 (1 reviews)

Cat. No.: HY-153220 Purity: 99.06%: FAQs
Data Sheet SDS COA Handling Instructions

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NX-2127 (compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTK^C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells. NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303). Among which, the conjugate of E3 ubiquitin ligase ligand + Linker compose of Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).

For research use only. We do not sell to patients.

NX-2127 Chemical Structure

CAS No. : 2416131-46-7

Size	Price	Stock	Quantity
5 mg	USD 330	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1040	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1660	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2650	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of NX-2127:

(R)-NX-2127 Get quote

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Description

NX-2127 (compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTK^C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells^[1]^[2]. NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303). Among which, the conjugate of E3 ubiquitin ligase ligand + Linker compose of Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).

In Vitro

NX-2127 inhibits proliferation of BTK-C481S mutant TMD8 cells with an EC₅₀ value <30 nM^[1].
NX-2127 increases IL-2 production in primary human T Cells^[1].

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

In Vivo

NX-2127 (1 mg/kg; po; once daily for 14 days) demonstrates potent degradation of BTK in cynomolgus monkeys in vivo^[1].
NX-2127 (po) leads to dose-proportional exposure in plasma and BTK degradation to <10% of baseline levels in circulating and splenic B cells^[1].
NX-2127 results in superior tumor growth inhibition (TGI) in both WT TMD8 and C481S mutant xenograft models in mouse^[1].

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

Clinical Trial

Molecular Weight

719.83

Formula

C₃₉H₄₅N₉O₅

CAS No.

2416131-46-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=CC(N3C[C@H](CN4CCC(C5=CC=C(C=C5)NC6=C(N=CC(N7CCCCC7)=N6)C(N)=O)CC4)CC3)=CC=C2C(N1C8C(NC(CC8)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (138.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3892 mL	6.9461 mL	13.8922 mL
5 mM	0.2778 mL	1.3892 mL	2.7784 mL
10 mM	0.1389 mL	0.6946 mL	1.3892 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.72%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (251 KB) HNMR (338 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Robbins D W, et al. Nx-2127, a degrader of BTK and IMiD neosubstrates, for the treatment of B-cell malignancies. Blood, 2020, 136: 34.

[2]. Mato A, et al. A first-in-human phase 1 trial of NX-2127, a first-in-class oral BTK degrader with IMiD-like activity, in patients with relapsed and refractory B-cell malignancies. 2022.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.3892 mL	6.9461 mL	13.8922 mL	34.7304 mL
	5 mM	0.2778 mL	1.3892 mL	2.7784 mL	6.9461 mL
	10 mM	0.1389 mL	0.6946 mL	1.3892 mL	3.4730 mL
	15 mM	0.0926 mL	0.4631 mL	0.9261 mL	2.3154 mL
	20 mM	0.0695 mL	0.3473 mL	0.6946 mL	1.7365 mL
	25 mM	0.0556 mL	0.2778 mL	0.5557 mL	1.3892 mL
	30 mM	0.0463 mL	0.2315 mL	0.4631 mL	1.1577 mL
	40 mM	0.0347 mL	0.1737 mL	0.3473 mL	0.8683 mL
	50 mM	0.0278 mL	0.1389 mL	0.2778 mL	0.6946 mL
	60 mM	0.0232 mL	0.1158 mL	0.2315 mL	0.5788 mL
	80 mM	0.0174 mL	0.0868 mL	0.1737 mL	0.4341 mL
	100 mM	0.0139 mL	0.0695 mL	0.1389 mL	0.3473 mL

NX-2127 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NX-21272416131-46-7NX2127NX 2127PROTACsBtkBruton tyrosine kinaseBTK-C481S mutantTMD8 cellsIL-2primary human T Cellscynomolgus monkeysWT TMD8 xenograft modelsC481S mutant xenograft modelsInhibitorinhibitorinhibit

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NX-2127

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