Cart summary

You have no items in your shopping cart.

Temuterkib

SKU: orb1303171

Description

Temuterkib (LY3214996) is an oral, potent, and selective ERK1/2 inhibitor with antineoplastic potential. It is used in cancer research, particularly for studying MAPK pathway-driven tumors, and has demonstrated activity in both in vitro cellular assays and in vivo xenograft models.

Research Area

Signal Transduction

Images & Validation

Key Properties

CAS Number1951483-29-6
MW453.56
Purity>99.99% (May vary between batches)
FormulaC22H27N7O2S
SMILESCn1nccc1Nc1nccc(n1)-c1cc2C(=O)N(CCN3CCOCC3)C(C)(C)c2s1
TargetERK
SolubilityDMSO:7.36 mg/mL (16.23 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.2 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

Target IC50
ERK2:5 nM|ERK1:5 nM
In Vivo
In tumor xenograft models, LY3214996 effectively inhibits the PD biomarker phospho-p90RSK1 and its PD effects, correlating with compound exposure and antitumor activity. It demonstrates comparable or superior efficacy to existing ERK inhibitors in BRAF or RAS mutant cell lines and xenografts. Oral administration of LY3214996 notably suppresses tumor growth across various cancer xenografts, including BRAF or NRAS mutant melanoma, and BRAF or KRAS mutant colorectal, lung, and pancreatic cancers, showing good tolerance. It offers a promising therapeutic strategy for cancers linked to MAPK pathway alterations. Remarkably, LY3214996 also counters Vemurafenib-resistant A375 melanoma xenografts, highlighting its potential in treating melanoma patients unresponsive to BRAF therapy. Furthermore, LY3214996 can be used alongside investigational and approved treatments, especially in KRAS mutant cases. Its combination with the CDK4/6 inhibitor abemaciclib exhibits significant tumor growth inhibition or regression in diverse cancer models, including KRAS mutant colorectal and non-small cell lung cancers, showcasing its broad therapeutic potential.
In Vitro
Temuterkib is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to Temuterkib.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

inhibit, LY3214996, LY-3214996, LY 3214996, Inhibitor, ERK1, ERK2, ERK, Extracellular signal regulated kinases, Temuterkib

Similar Products

  • LY-3214996 [orb1225789]

    >98% (HPLC)

    1951483-29-6

    453.56

    C22H27N7O2S

    25 mg, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg, 1 g, 500 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Key Properties

No computed properties available.

Documents Download

Datasheet
Product Information
Download

Request a Document

Protocol Information

Temuterkib (orb1303171)

  • Star
  • Star
  • Star
  • Star
  • Star
  • 0.0
Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

Login to Submit a Review

No reviews yet

Step 1: Enter information below

(Recommended: An additional animal making an allowance for loss during the experiment)

Step 2: Enter the in vivo formulation

(This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 100.00
2 mg
$ 120.00
5 mg
$ 150.00
1 ml x 10 mM (in DMSO)
$ 160.00
10 mg
$ 220.00
25 mg
$ 430.00
50 mg
$ 630.00
100 mg
$ 870.00
DispatchUsually dispatched within 3-5 working days
Bulk Enquiry