TH-Z827

Cat. No.: HY-153663 Purity: 95.12%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC₅₀ of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC₅₀ value of 42 μM.

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

TH-Z827 Chemical Structure

CAS No. : 2847881-81-4

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5 mg		Ask For Quote & Lead Time
10 mg		Ask For Quote & Lead Time
25 mg		Ask For Quote & Lead Time
50 mg		Ask For Quote & Lead Time
100 mg		Ask For Quote & Lead Time

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This product is a controlled substance and not for sale in your territory.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

KRAS(G12D)

2.4 μM (IC₅₀)

In Vitro

In two pancreatic cancer cell lines bearing the KRAS G12D mutation (PANC-1 and Panc 04.03), TH-Z827 conferres anti-proliferative effects with IC₅₀ values of 4.4 and 4.7 μM, respectively. Treatment with TH-Z827 also reduces the levels of pERK and pAKT in PANC-1 and Panc 04.03 cells, confirming that TH-Z827 prevents the activation of MAPK and PI3K/mTOR signaling^[1].

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

In Vivo

BALB/c nude mice subcutaneously inoculated with Panc 04.03 cells and C57BL/6 mice inoculated with KPC cells. In the nude mice model, TH-Z827 (10-30 mg/kg) significantly reduces the tumor volumes, and does so in a dose-dependent manner. However, an intraperitoneal dosing of 30 mg/kg TH-Z827 results in observed weight loss, again suggesting the potential of off-target effects^[1].

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

Molecular Weight

498.66

Formula

C₃₀H₃₈N₆O

CAS No.

2847881-81-4

Appearance

Solid

Color

White to off-white

SMILES

CN(CCC1)[C@@H]1COC2=NC(N3[C@@H]4CNC[C@H]3CC4)=C5C(CN(C6=CC=CC7=C6C(C)=CC=C7)CC5)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (200.54 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	2.0054 mL	10.0269 mL	20.0537 mL
5 mM	0.4011 mL	2.0054 mL	4.0107 mL
10 mM	0.2005 mL	1.0027 mL	2.0054 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 95.12%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (252 KB) HNMR (138 KB) RP-HPLC (162 KB) NP-HPLC (126 KB) LCMS (107 KB)

Handling Instructions (2659 KB)

References

[1]. Zhongwei Mao, et al. KRAS(G12D) can be targeted by potent inhibitors via formation of salt bridge. Cell Discov. 2022 Jan 25;8(1):5. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.0054 mL	10.0269 mL	20.0537 mL	50.1344 mL
	5 mM	0.4011 mL	2.0054 mL	4.0107 mL	10.0269 mL
	10 mM	0.2005 mL	1.0027 mL	2.0054 mL	5.0134 mL
	15 mM	0.1337 mL	0.6685 mL	1.3369 mL	3.3423 mL
	20 mM	0.1003 mL	0.5013 mL	1.0027 mL	2.5067 mL
	25 mM	0.0802 mL	0.4011 mL	0.8021 mL	2.0054 mL
	30 mM	0.0668 mL	0.3342 mL	0.6685 mL	1.6711 mL
	40 mM	0.0501 mL	0.2507 mL	0.5013 mL	1.2534 mL
	50 mM	0.0401 mL	0.2005 mL	0.4011 mL	1.0027 mL
	60 mM	0.0334 mL	0.1671 mL	0.3342 mL	0.8356 mL
	80 mM	0.0251 mL	0.1253 mL	0.2507 mL	0.6267 mL
	100 mM	0.0201 mL	0.1003 mL	0.2005 mL	0.5013 mL

TH-Z827 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:

TH-Z8272847881-81-4RasKRAS(G12D) inhibitorKRAS(G12D)-CRAFanti-proliferative effects pERKpAKTInhibitorinhibitorinhibit

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